2088715-91-5

中文名称化合物 MFH290

英文名称 2-Propenamide, N-[4-[[(3R)-3-[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]-1-piperidinyl]carbonyl]phenyl]-

CAS 2088715-91-5

分子式 C26H31N5O3S2

分子量 525.69

MOL 文件 2088715-91-5.mol

2088715-91-5 结构式

基本信息物理化学性质应用领域常见问题列表

基本信息

中文别名

化合物 MFH290

英文别名

MFH290
2-Propenamide, N-[4-[[(3R)-3-[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]-1-piperidinyl]carbonyl]phenyl]-

物理化学性质

密度1.31±0.1 g/cm3(Predicted)

酸度系数(pKa)13.29±0.70(Predicted)

形态Solid

颜色White to off-white

应用领域

用途一

MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.

常见问题列表

概述

MFH290 是一种有效的高选择性细胞周期蛋白依赖性激酶 12/13 (CDK12/13) 共价抑制剂。MFH290 与 CDK12 的 Cys-1039 形成共价键，表现出优异的 kinome 选择性，抑制 -聚合酶II (Pol II) C-terminal domain (CTD)中丝氨酸-2的磷酸化。MFH290用于癌症研究。