DNA Methyltransferase

信号通路图

研究领域

抑制剂选择性比较

DNA Methyltransferase产品

所有产品 DNA Methyltransferase抑制剂(8)

产品目录	产品描述	文献引用	实验数据
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）。	Nat Biotechnol, 2019, 10.1038/s41587-019-0372-z Nat Med, 2019, 25(7):1073-1081 Cancer Discov, 2019, 9(1):34-45	(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,5-AzaC,Ladakamycin) Azacitidine 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。	J Clin Invest, 2019, 10.1172/JCI128571 Cancer Immunol Res, 2019, 7(2):230-243 J Immunother Cancer, 2019, 7(1):277	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。	Exp Cell Res, 2020, 386(2):111743 Toxicol Appl Pharmacol, 2019, 378:114606 Cell Physiol Biochem, 2018, 50(4):1376-1397	The inhibition effect of RG108 on M.SssI MTase activity.
S7113	Zebularine Zebularine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。	New Phytol, 2018, 220(2):476-487 Plant Biotechnol J, 2018, 10.1111/pbi.12988 Nucleic Acids Res, 2016, 44(9):4067-79	(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 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。	Cell Rep, 2019, 27(11):3331-3344
S7276	SGI-1027 SGI-1027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。	Cell Mol Biol Lett, 2019, 24:10 Oncol Lett, 2018, 16(5):5799-5806 J Clin Invest, 2016, 126(10):3961-3980	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.
S2250	(-)-Epigallocatechin Gallate (-)-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。	Oncogene, 2019, 38(15):2690-2705 Onco Targets Ther, 2019, 12:6033-6043 Exp Ther Med, 2018, 15(5):4284-4290
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。

产品目录	产品描述	文献引用	实验数据
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）。	Nat Biotechnol,2019, 10.1038/s41587-019-0372-z Nat Med,2019, 25(7):1073-1081 Cancer Discov,2019, 9(1):34-45	(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,5-AzaC,Ladakamycin) Azacitidine 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。	J Clin Invest,2019, 10.1172/JCI128571 Cancer Immunol Res,2019, 7(2):230-243 J Immunother Cancer,2019, 7(1):277	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。	Exp Cell Res,2020, 386(2):111743 Toxicol Appl Pharmacol,2019, 378:114606 Cell Physiol Biochem,2018, 50(4):1376-1397	The inhibition effect of RG108 on M.SssI MTase activity.
S7113	Zebularine Zebularine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。	New Phytol,2018, 220(2):476-487 Plant Biotechnol J,2018, 10.1111/pbi.12988 Nucleic Acids Res,2016, 44(9):4067-79	(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 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。	Cell Rep,2019, 27(11):3331-3344
S7276	SGI-1027 SGI-1027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。	Cell Mol Biol Lett,2019, 24:10 Oncol Lett,2018, 16(5):5799-5806 J Clin Invest,2016, 126(10):3961-3980	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.
S2250	(-)-Epigallocatechin Gallate (-)-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。	Oncogene,2019, 38(15):2690-2705 Onco Targets Ther,2019, 12:6033-6043 Exp Ther Med,2018, 15(5):4284-4290
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。