Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate 是一种选择性的组蛋白甲基转移酶 SETD7 抑制剂 (IC50 = 4.59 μM),具有抗癌活性。
产品描述
Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.
体外活性
Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate (0-100 μM) inhibits the proliferation of MCF7, HL60 and MV4-11 cells in a dose-dependent manner with the IC50 values of 10.93 μM and 16.43 μM, respectively. Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate inhibits DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a by less than 45%, whereas it inhibits SET7 by 90% at concentrations of 100 μM[1].
Cas No.
303141-21-1
分子式
C15H15N3O5S
分子量
349.36
别名
DC-S239
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years