DNA Methyltransferase

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

DNA Methyltransferase产品

所有产品(14) DNA Methyltransferase抑制剂(14)

目录号	产品描述	文献引用	实验数据
S1200	Decitabine (NSC 127716) Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR)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。	Cell Stem Cell, 2022, S1934-5909(22)00010-8 Signal Transduct Target Ther, 2022, 7(1):35 EMBO Mol Med, 2022, 14(2):e14903	(A) and (B) SW1116 and LOVO cells were plated, treated for 48 h with decitabine (DAC) and gefitinib (GEF) either alone or in combination, and the expression levels of AKT, mTOR, S6K, and phosphorylation were determined by Western blot analysis as described under Methods. Expression of β-actin served as a loading control. The data are representative of three independent experiments.
S1782	Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486) 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。	Cancer Discov, 2022, candisc.1117.2021 Signal Transduct Target Ther, 2022, 7(1):147 Front Oncol, 2022, 12:832816	R-2HG treatment or chemotherapeutic treatment, especially their combinations, decrease MYC levels in leukemic cells (using MONOMAC-6 as a representative). AZA:Azacitidine.
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。	Int J Mol Sci, 2022, 23(8)4213 Front Oncol, 2021, 11:773186 Cell Biol Toxicol, 2021, 10.1007/s10565-021-09596-y	The inhibition effect of RG108 on M.SssI MTase activity.
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K_i为2 μM。	Cell Death Dis, 2021, 12(11):1046 Pain, 2020, 161(1):96-108 J Neuroendocrinol, 2020, 32(2):e12819	(A) Zebularine treatment suppresses fibre development in vitro. This figure shows that 0 day post anthesis (DPA) ovules cultured for 10 days exhibit different fibre lengths. Different concentrations of zebularine (20, 40 and 80 μM) were applied.
S1774	Thioguanine (NSC 752) Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol) 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。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Nat Commun, 2021, 12(1):4961 Microbiol Spectr, 2021, 9(3):e0064621
E1046^New	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。
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。	Head Neck, 2022, 44(5):1192-1205 Oxid Med Cell Longev, 2021, 2021:5550196 J Ethnopharmacol, 2021, 281:114559	Following the incubation of the unmethylated DNA probe with DNMTase in the presence of spotted DNMTIs, Cy5 intensity values were measured before ( I₀ ) and after ( I₃₀ ) of endonuclease cleavage. Each data set was normalized to the initial fluorescence signal within the corresponding block and the resulting ratio describes the net CpG sites remained uncleaved (盨.D., n = 64). The red line represents the inhibitory threshold determined as two standard deviations below the averaged 'unspotted' ratio. On-chip visualization of the corresponding remaining Cy5 signal is placed on the bottom of each column.
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.	Cell Death Dis, 2021, 12(2):188
S2250	(-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) 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。	Exp Cell Res, 2022, 411(1):113000 Int J Mol Med, 2022, 49(1)11 EMBO Rep, 2021, e53166
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。	Front Neurol, 2021, 12:652882 Cancer Cell Int, 2020, 20:363
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。	Nat Med, 2019, 25(7):1073-1081
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.
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。
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。

目录号	产品描述	文献引用	实验数据
S1200	Decitabine (NSC 127716) Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR)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。	Cell Stem Cell,2022, S1934-5909(22)00010-8 Signal Transduct Target Ther,2022, 7(1):35 EMBO Mol Med,2022, 14(2):e14903	(A) and (B) SW1116 and LOVO cells were plated, treated for 48 h with decitabine (DAC) and gefitinib (GEF) either alone or in combination, and the expression levels of AKT, mTOR, S6K, and phosphorylation were determined by Western blot analysis as described under Methods. Expression of β-actin served as a loading control. The data are representative of three independent experiments.
S1782	Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486) 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。	Cancer Discov,2022, candisc.1117.2021 Signal Transduct Target Ther,2022, 7(1):147 Front Oncol,2022, 12:832816	R-2HG treatment or chemotherapeutic treatment, especially their combinations, decrease MYC levels in leukemic cells (using MONOMAC-6 as a representative). AZA:Azacitidine.
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。	Int J Mol Sci,2022, 23(8)4213 Front Oncol,2021, 11:773186 Cell Biol Toxicol,2021, 10.1007/s10565-021-09596-y	The inhibition effect of RG108 on M.SssI MTase activity.
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K_i为2 μM。	Cell Death Dis,2021, 12(11):1046 Pain,2020, 161(1):96-108 J Neuroendocrinol,2020, 32(2):e12819	(A) Zebularine treatment suppresses fibre development in vitro. This figure shows that 0 day post anthesis (DPA) ovules cultured for 10 days exhibit different fibre lengths. Different concentrations of zebularine (20, 40 and 80 μM) were applied.
S1774	Thioguanine (NSC 752) Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol) 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。	Hum Cell,2022, 10.1007/s13577-022-00671-y Nat Commun,2021, 12(1):4961 Microbiol Spectr,2021, 9(3):e0064621
E1046^New	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。
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。	Head Neck,2022, 44(5):1192-1205 Oxid Med Cell Longev,2021, 2021:5550196 J Ethnopharmacol,2021, 281:114559	Following the incubation of the unmethylated DNA probe with DNMTase in the presence of spotted DNMTIs, Cy5 intensity values were measured before ( I₀ ) and after ( I₃₀ ) of endonuclease cleavage. Each data set was normalized to the initial fluorescence signal within the corresponding block and the resulting ratio describes the net CpG sites remained uncleaved (盨.D., n = 64). The red line represents the inhibitory threshold determined as two standard deviations below the averaged 'unspotted' ratio. On-chip visualization of the corresponding remaining Cy5 signal is placed on the bottom of each column.
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.	Cell Death Dis,2021, 12(2):188
S2250	(-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) 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。	Exp Cell Res,2022, 411(1):113000 Int J Mol Med,2022, 49(1)11 EMBO Rep,2021, e53166
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。	Front Neurol,2021, 12:652882 Cancer Cell Int,2020, 20:363
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。	Nat Med,2019, 25(7):1073-1081
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.
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。
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。