CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation.
CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation.
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