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Apexbio Technology LLC THZ531 1702809-17-3 25mg
Supplier: Apexbio Technology LLC A873625
THZ531 (CAS 1702809-17-3) is a covalent inhibitor of cyclin-dependent kinase 12 (CDK12) and CDK13 These kinases in complex with cyclin K mediate transcription elongation and RNA processing through phosphorylation of RNA polymerase II (Pol II) THZ531 irreversibly binds to CDK12 and CDK13 exhibiting inhibitory potency (IC50) of 158 nM and 69 nM respectively while showing substantially lower affinity ( 50-fold) toward related CDK7 and CDK9 In Jurkat cells THZ531 induces apoptosis and impairs proliferation (IC50 50 nM) reducing Pol II Ser2 phosphorylation and inhibiting transcription of certain super-enhancer-linked and DNA damage response genes THZ531 serves as a research tool to investigate transcriptional regulation and associated oncogenic pathways
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