YKL-5-124

YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA polymerase II phosphorylation status.