| S1200 | 
                                
                                    
                                    Decitabine
                                
                                 | 
                                Decitabine是DNA甲基转移酶抑制剂,整合进入DNA、导致DNA低甲基化,并使DNA复制停滞在intra-S-phase。Decitabine被用于治疗骨髓增生异常综合征(MDS)。Decitabine可在多种癌细胞系中诱导细胞周期阻滞和凋亡。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Cancer Cell, 2025, S1535-6108(25)00223-5
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nat Commun, 2025, 16(1):4451
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cell Rep Med, 2025, S2666-3791(25)00102-8
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S1782 | 
                                
                                    
                                    Azacitidine (5-Azacytidine)
                                
                                 | 
                                Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷类似物,通过捕获DNA甲基转移酶,特异性抑制DNA甲基化。Azacitidine可诱导线粒体凋亡与自噬。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Mol Cancer, 2025, 24(1):154
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cell Rep Med, 2025, S2666-3791(25)00102-8
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    J Exp Clin Cancer Res, 2025, 44(1):10
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S2250 | 
                                
                                    
                                    EGCG ((-)-Epigallocatechin Gallate)
                                
                                 | 
                                EGCG ((-)-Epigallocatechin Gallate)是从绿茶中分离的一种有效的抗氧化剂Polyphenol flavonoid。抑制telomerase和DNA methyltransferase, 阻滞EGF受体和HER-2受体的激活,抑制脂肪酸合成酶以及谷氨酸脱氢酶的活性。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cell Rep, 2025, 44(6):115799
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Front Pharmacol, 2024, 15:1403424
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S2821 | 
                                
                                    
                                    RG108
                                
                                 | 
                                RG108 (N-Phthalyl-L-tryptophan)是一种DNA methyltransferase抑制剂,无细胞试验中IC50为115 nM,不会引起共价酶的诱捕。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    J Transl Med, 2025, 23(1):193
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cells, 2025, 14(2)135
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Neural Regen Res, 2024, 19(10):2229-2239
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S1774 | 
                                
                                    
                                    Thioguanine
                                
                                 | 
                                Thioguanine是一种嘌呤类的抗代谢药物,抑制了DNMT1的活性,广泛用于治疗急性淋巴细胞白血病,自身免疫性疾病(如克罗恩氏病,类风湿关节炎)和器官移植接受患者。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    BMC Microbiol, 2025, 25(1):53
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Gastroenterology, 2024, S0016-5085(24)00062-3
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    iScience, 2024, 27(10):110862
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S7276 | 
                                
                                    
                                    SGI-1027
                                
                                 | 
                                SGI-1027 (DNA Methyltransferase Inhibitor II) 是一种DNMT抑制剂,作用于DNMT1,DNMT3A和DNMT3B,无细胞试验中IC50分别为6,8和7.5 μM。SGI‑1027 可诱导凋亡。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Eur J Pharm Sci, 2024, 197:106767
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Parasites Hosts Dis, 2024, 62(1):98-116
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Int J Biol Sci, 2022, 18(11):4372-4387
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S7113 | 
                                
                                    
                                    Zebularine (NSC 309132)
                                
                                 | 
                                Zebularine (NSC 309132, 4-Deoxyuridine)是一种DNA methylation抑制剂,与DNA methyltransferases形成共价复合物,也抑制胞苷脱氨酶,无细胞试验中Ki为2 μM。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Insect Mol Biol, 2024, 10.1111/imb.12933
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Leukemia, 2022, 10.1038/s41375-022-01746-3
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    J Transl Med, 2022, 20(1):383
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                        
                                             
                                        
                                    
                                 | 
                            
                        
                            
                                | S3957 | 
                                
                                    
                                    Gamma-Oryzanol
                                
                                 | 
                                Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. | 
                                
                                    
                                        
                                            
                                                - 
                                                    PLoS One, 2024, 19(5):e0302745
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nutrients, 2023, 15(16)3630
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nutrients, 2023, 15(16)3630
                                                
 
                                             
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S6682 | 
                                
                                    
                                    Bobcat339 hydrochloride
                                
                                 | 
                                Bobcat339是一种选择性的基于胞嘧啶的TET enzyme抑制剂,对于TET1 和 TET2的IC50分别为33 μM和73 μM。Bobcat339可通过抑制活细胞中的TET酶功能来降低DNA 5-羟甲基胞嘧啶的丰度,并为其实用的药理探针提供支持。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cell Death Dis, 2024, 15(8):617
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Cell Commun Signal, 2024, 22(1):95
                                                
 
                                             
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S8812 | 
                                
                                    
                                    CM272
                                
                                 | 
                                CM272是新型、一流的G9a (GLP) 和 DNMTs双重可逆抑制剂,对G9a, DNMT1, DNMT3A, DNMT3B, GLP的IC50值分别为8 nM, 382 nM, 85 nM, 1200 nM, 2 nM。CM272通过至少部分诱导免疫原性细胞死亡,延长了血液系统恶性肿瘤体内模型的存活时间。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Hepatol Commun, 2024, 8(2)e0378
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nat Med, 2019, 25(7):1073-1081
                                                
 
                                             
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | E1046 | 
                                
                                    
                                    GSK3685032
                                
                                 | 
                                GSK3685032是一种非时间依赖性、高度选择性的 DNA 甲基转移酶 (DNMT1) 抑制剂,IC50值为0.036 μM,其作用于DNMT1比作用于DNMT3A/3L 和 DNMT3B/3L选择性高2500倍。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    NPJ Precis Oncol, 2025, 9(1):62
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nat Commun, 2024, 15(1):7360
                                                
 
                                             
                                        
                                    
                                        
                                            
                                                - 
                                                    Nat Commun, 2023, 14(1):3966
                                                
 
                                             
                                        
                                    
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S4771 | 
                                
                                    
                                    β-thujaplicin
                                
                                 | 
                                β-Thujaplicin (β-TH, Hinokitiol, 4-Isopropyltropolone) is a toxic tropolone derivative present in the heartwood of western red cedar (Thuja plicata) and is used as a preservative and antimicrobial additive in a number of commercial goods. Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities. | 
                                
                                    
                                        
                                            
                                                - 
                                                    Invest New Drugs, 2022, 10.1007/s10637-022-01229-3
                                                
 
                                             
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | F0279 | 
                                
                                    
                                        
                                            DNMT1 Antibody [F10L24]
                                        
                                    
                                 | 
                                DNMT1 Rabbit mAb recognizes endogenous levels of total DNMT1 protein. | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | F1036 | 
                                
                                    
                                        
                                            Dnmt3a Antibody [L22H18]
                                        
                                    
                                 | 
                                 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | F0001 | 
                                
                                    
                                        
                                            DNMT3B Antibody [B16G3]
                                        
                                    
                                 | 
                                 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | F2976New | 
                                
                                    
                                        
                                            SF3B1 Antibody [G23D1]
                                        
                                    
                                 | 
                                 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | E1556 | 
                                
                                    
                                    GSK-3484862
                                
                                 | 
                                GSK-3484862 是一种非共价、强效且选择性的DNMT1抑制剂,其IC50为 0.23 μM。它在急性髓系白血病中显示出疗效。 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | E4795New | 
                                
                                    
                                    Bobcat339
                                
                                 | 
                                Bobcat339 是一种胞嘧啶类小分子 TET 酶 抑制剂,对 TET1 和 TET2 的 IC50 分别为 33 μM 和 73 μM,可降低海马神经元中的 DNA 5hmC 水平。它可用于表观遗传学研究,是针对 DNA 甲基化和基因转录的疗法的潜在起点。 | 
                                
                                    
                                        
                                            
                                                - 
                                                    Biomater Res, 2025, 29:0229
                                                
 
                                             
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S3543 | 
                                
                                    
                                    DC-05
                                
                                 | 
                                DC-05为DNA甲基转移酶1(DNA methyltransferase 1, DNMT1)抑制剂,IC50为10.3 μM, Kd为1.09 μM。 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S4294 | 
                                
                                    
                                    Procainamide HCl
                                
                                 | 
                                Procainamide HCl是一种sodium channel的阻断剂,也是DNA甲基转移酶抑制剂,用于心律失常的治疗。
 | 
                                
                                    
                                        
                                            
                                                - 
                                                    J Immunother Cancer, 2024, 12(11)e009805
                                                
 
                                             
                                        
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                            
                                | S2477 | 
                                
                                    
                                    2'-Deoxy-5-Fluorocytidine
                                
                                 | 
                                2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR)是一种嘧啶类似物,是目前应用于实体瘤临床试验中的一种 DNA methyltransferase (DMNT) 抑制剂。 | 
                                
                                    
                                 | 
                                
                                    
                                 | 
                            
                        
                        
                    
                    
                        
                        
                            
                        
                            
                                
                                    
                                        | S1200 | 
                                        
                                            Decitabine
                                         | 
                                        Decitabine是DNA甲基转移酶抑制剂,整合进入DNA、导致DNA低甲基化,并使DNA复制停滞在intra-S-phase。Decitabine被用于治疗骨髓增生异常综合征(MDS)。Decitabine可在多种癌细胞系中诱导细胞周期阻滞和凋亡。 | 
                                        
                                            
                                                
                                                    
                                                        - Cancer Cell, 2025, S1535-6108(25)00223-5
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nat Commun, 2025, 16(1):4451
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cell Rep Med, 2025, S2666-3791(25)00102-8
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                         | 
                                        
                                            
                                                
                                                     
                                                
                                            
                                         | 
                                    
                                
                                    
                                        | S1782 | 
                                        
                                            Azacitidine (5-Azacytidine)
                                         | 
                                        Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷类似物,通过捕获DNA甲基转移酶,特异性抑制DNA甲基化。Azacitidine可诱导线粒体凋亡与自噬。 | 
                                        
                                            
                                                
                                                    
                                                        - Mol Cancer, 2025, 24(1):154
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cell Rep Med, 2025, S2666-3791(25)00102-8
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - J Exp Clin Cancer Res, 2025, 44(1):10
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
   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                                         | 
                                    
                                
                                    
                                        | S2250 | 
                                        
                                            EGCG ((-)-Epigallocatechin Gallate)
                                         | 
                                        EGCG ((-)-Epigallocatechin Gallate)是从绿茶中分离的一种有效的抗氧化剂Polyphenol flavonoid。抑制telomerase和DNA methyltransferase, 阻滞EGF受体和HER-2受体的激活,抑制脂肪酸合成酶以及谷氨酸脱氢酶的活性。 | 
                                        
                                            
                                                
                                                    
                                                        - Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cell Rep, 2025, 44(6):115799
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Front Pharmacol, 2024, 15:1403424
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                         | 
                                        
                                            
                                                
                                                     
                                                
                                            
                                         | 
                                    
                                
                                    
                                        | S2821 | 
                                        
                                            RG108
                                         | 
                                        RG108 (N-Phthalyl-L-tryptophan)是一种DNA methyltransferase抑制剂,无细胞试验中IC50为115 nM,不会引起共价酶的诱捕。 | 
                                        
                                            
                                                
                                                    
                                                        - J Transl Med, 2025, 23(1):193
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cells, 2025, 14(2)135
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Neural Regen Res, 2024, 19(10):2229-2239
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
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                                         | 
                                    
                                
                                    
                                        | S1774 | 
                                        
                                            Thioguanine
                                         | 
                                        Thioguanine是一种嘌呤类的抗代谢药物,抑制了DNMT1的活性,广泛用于治疗急性淋巴细胞白血病,自身免疫性疾病(如克罗恩氏病,类风湿关节炎)和器官移植接受患者。 | 
                                        
                                            
                                                
                                                    
                                                        - BMC Microbiol, 2025, 25(1):53
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Gastroenterology, 2024, S0016-5085(24)00062-3
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - iScience, 2024, 27(10):110862
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
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                                         | 
                                    
                                
                                    
                                        | S7276 | 
                                        
                                            SGI-1027
                                         | 
                                        SGI-1027 (DNA Methyltransferase Inhibitor II) 是一种DNMT抑制剂,作用于DNMT1,DNMT3A和DNMT3B,无细胞试验中IC50分别为6,8和7.5 μM。SGI‑1027 可诱导凋亡。 | 
                                        
                                            
                                                
                                                    
                                                        - Eur J Pharm Sci, 2024, 197:106767
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Parasites Hosts Dis, 2024, 62(1):98-116
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Int J Biol Sci, 2022, 18(11):4372-4387
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
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                                         | 
                                    
                                
                                    
                                        | S7113 | 
                                        
                                            Zebularine (NSC 309132)
                                         | 
                                        Zebularine (NSC 309132, 4-Deoxyuridine)是一种DNA methylation抑制剂,与DNA methyltransferases形成共价复合物,也抑制胞苷脱氨酶,无细胞试验中Ki为2 μM。 | 
                                        
                                            
                                                
                                                    
                                                        - Insect Mol Biol, 2024, 10.1111/imb.12933
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Leukemia, 2022, 10.1038/s41375-022-01746-3
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - J Transl Med, 2022, 20(1):383
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
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                                        | S3957 | 
                                        
                                            Gamma-Oryzanol
                                         | 
                                        Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. | 
                                        
                                            
                                                
                                                    
                                                        - PLoS One, 2024, 19(5):e0302745
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nutrients, 2023, 15(16)3630
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nutrients, 2023, 15(16)3630
 
                                                     
                                                
                                            
                                                
                                            
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                                        | S6682 | 
                                        
                                            Bobcat339 hydrochloride
                                         | 
                                        Bobcat339是一种选择性的基于胞嘧啶的TET enzyme抑制剂,对于TET1 和 TET2的IC50分别为33 μM和73 μM。Bobcat339可通过抑制活细胞中的TET酶功能来降低DNA 5-羟甲基胞嘧啶的丰度,并为其实用的药理探针提供支持。 | 
                                        
                                            
                                                
                                                    
                                                        - Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cell Death Dis, 2024, 15(8):617
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Cell Commun Signal, 2024, 22(1):95
 
                                                     
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
                                                
                                            
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                                        | S8812 | 
                                        
                                            CM272
                                         | 
                                        CM272是新型、一流的G9a (GLP) 和 DNMTs双重可逆抑制剂,对G9a, DNMT1, DNMT3A, DNMT3B, GLP的IC50值分别为8 nM, 382 nM, 85 nM, 1200 nM, 2 nM。CM272通过至少部分诱导免疫原性细胞死亡,延长了血液系统恶性肿瘤体内模型的存活时间。 | 
                                        
                                            
                                                
                                                    
                                                        - Hepatol Commun, 2024, 8(2)e0378
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nat Med, 2019, 25(7):1073-1081
 
                                                     
                                                
                                            
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                                        | E1046 | 
                                        
                                            GSK3685032
                                         | 
                                        GSK3685032是一种非时间依赖性、高度选择性的 DNA 甲基转移酶 (DNMT1) 抑制剂,IC50值为0.036 μM,其作用于DNMT1比作用于DNMT3A/3L 和 DNMT3B/3L选择性高2500倍。 | 
                                        
                                            
                                                
                                                    
                                                        - NPJ Precis Oncol, 2025, 9(1):62
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nat Commun, 2024, 15(1):7360
 
                                                     
                                                
                                            
                                                
                                                    
                                                        - Nat Commun, 2023, 14(1):3966
 
                                                     
                                                
                                            
                                                
                                            
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                                        | S4771 | 
                                        
                                            β-thujaplicin
                                         | 
                                        β-Thujaplicin (β-TH, Hinokitiol, 4-Isopropyltropolone) is a toxic tropolone derivative present in the heartwood of western red cedar (Thuja plicata) and is used as a preservative and antimicrobial additive in a number of commercial goods. Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities. | 
                                        
                                            
                                                
                                                    
                                                        - Invest New Drugs, 2022, 10.1007/s10637-022-01229-3
 
                                                     
                                                
                                            
                                         | 
                                        
                                            
                                         | 
                                    
                                
                                    
                                        | E1556 | 
                                        
                                            GSK-3484862
                                         | 
                                        GSK-3484862 是一种非共价、强效且选择性的DNMT1抑制剂,其IC50为 0.23 μM。它在急性髓系白血病中显示出疗效。 | 
                                        
                                            
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                                        | E4795New | 
                                        
                                            Bobcat339
                                         | 
                                        Bobcat339 是一种胞嘧啶类小分子 TET 酶 抑制剂,对 TET1 和 TET2 的 IC50 分别为 33 μM 和 73 μM,可降低海马神经元中的 DNA 5hmC 水平。它可用于表观遗传学研究,是针对 DNA 甲基化和基因转录的疗法的潜在起点。 | 
                                        
                                            
                                                
                                                    
                                                        - Biomater Res, 2025, 29:0229
 
                                                     
                                                
                                            
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                                        | S3543 | 
                                        
                                            DC-05
                                         | 
                                        DC-05为DNA甲基转移酶1(DNA methyltransferase 1, DNMT1)抑制剂,IC50为10.3 μM, Kd为1.09 μM。 | 
                                        
                                            
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                                         | 
                                    
                                
                                    
                                        | S4294 | 
                                        
                                            Procainamide HCl
                                         | 
                                        Procainamide HCl是一种sodium channel的阻断剂,也是DNA甲基转移酶抑制剂,用于心律失常的治疗。
 | 
                                        
                                            
                                                
                                                    
                                                        - J Immunother Cancer, 2024, 12(11)e009805
 
                                                     
                                                
                                            
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                                        | S2477 | 
                                        
                                            2'-Deoxy-5-Fluorocytidine
                                         | 
                                        2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR)是一种嘧啶类似物,是目前应用于实体瘤临床试验中的一种 DNA methyltransferase (DMNT) 抑制剂。 | 
                                        
                                            
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