THZ531

Cdk12和Cdk13的抑制剂（Cdk12/cyclin K和Cdk13/cyclin K的IC50分别为158和69nM）；对Cdk12/cyclin K和Cdk13/cyclin K的选择性优于Cdk9/cyclin T1和Cdk7/cyclin H/MAT1（IC50分别为10.5和8.5μM）；抑制Jurkat细胞增殖（IC50=50nM）；以浓度依赖性方式诱导Jurkat细胞凋亡；在50nM浓度下降低Jurkat细胞中与DNA损伤反应相关的基因的表达，包括BRCA1、FANCF和ERCC4。An inhibitor of Cdk12 and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K, respectively); selective for Cdk12/cyclin K and Cdk13/cyclin K over Cdk9/cyclin T1 and Cdk7/cyclin H/MAT1 (IC50s = 10.5 and 8.5 μM, respectively); inhibits proliferation of Jurkat cells (IC50 = 50 nM); induces apoptosis in Jurkat cells in a concentration-dependent manner; reduces expression of genes associated with the DNA damage response, including BRCA1, FANCF, and ERCC4, in Jurkat cells at 50 nM.