产品描述:
THZ531 is an inhibitor of cyclin-dependent kinase 12 (Cdk12) and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K, respectively).{48369} It is 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). THZ531 inhibits proliferation of Jurkat cells with an IC50 value of 50 nM and induces apoptosis in a concentration-dependent manner. It also reduces expression of genes associated with the DNA damage response, including BRCA1, FANCF, and ERCC4, in Jurkat cells when used at a concentration of 50 nM.