cdk7/cych/mat1

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.

YKL-5-124 TFA, a potent and selective irreversible covalent inhibitor of CDK7, demonstrates IC50 values of 53.5 nM for CDK7 and 9.7 nM for the CDK7 Mat1 CycH complex. It exhibits over 100-fold selectivity for CDK7 over CDK9 and CDK2, while showing no activity against CDK12 and CDK13. This compound effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on the phosphorylation status of RNA polymerase II.

YKL-5-124 TFA is a potent, selective, irreversible and covalent inhibitor of CDK7 (IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7 Mat1 CycH, respectively).

YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7 Mat1 CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12 13.