THZ-531

Description	THZ531 is a covalent CDK12 and CDK13 covalent inhibitor. Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription. THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes. THZ531 dramatically induced apoptotic cell death. Small molecules capable of specifically targeting CDK12 and CDK13 may thus help identify cancer subtypes that are particularly dependent on their kinase activities.
Pathways	Cell Cycle/DNA Damage
Targets	CDK

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