Apexbio Technology LLC THZ1 Hydrochloride 1604810-83-4 (free base) 10mM (in 1mL DMSO)

Supplier:  Apexbio Technology LLC B47365.1

THZ1 Hydrochloride is a covalent inhibitor targeting the cyclin-dependent kinase CDK7 with an IC50 of approximately 3 2 nM Mechanistically THZ1 modifies CDK7 by covalently binding to a cysteine residue located outside the kinase domain thereby inhibiting kinase-mediated phosphorylation events associated with the RNA Polymerase II C-terminal domain (CTD) It perturbs transcriptional regulation pathways mediated by CDK7-related signaling in cells including inhibition of phosphorylation essential for initiation and elongation processes THZ1 has demonstrated inhibitory activity in various cancer cell lines particularly in T-cell acute lymphoblastic leukemia (T-ALL) cell lines such as Jurkat and Loucy where sensitivity correlates with interference of RUNX1 transcriptional programs THZ1 is primarily used as a pharmacological tool to investigate CDK7-driven transcriptional regulation and tumor biology

Catalog No. 50-000-62718