YKL-5-124 is a potent and highly selective covalent inhibitor of cyclin-dependent kinase 7 (CDK7) that induces cell cycle arrest at the G1/S transition.
potent and highly selective covalent inhibitor of cyclin-dependent kinase 7 (CDK7)
Cell chemical biology, 26(6), 792-803 (2019-03-25)
Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and transcription, but its precise role remains elusive. We previously described THZ1, a CDK7 inhibitor, which dramatically inhibits superenhancer-associated gene expression. However, potent CDK12/13 off-target activity obscured CDK7s contribution to this phenotype.
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