Pricing updated 2019-04-24. Prices are subject to change without notice.
THZ1 is a Cdk7 inhibitor (IC50s = 3.2-15.6 nM in vitro) that selectively targets a remote cysteine residue located outside of the classic kinase domain.1 THZ1 also targets Cdk12 kinase activity although at a higher concentration (IC50 = 250 nM).1 It displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines that display characteristic misregulation of T cell lineage-specific transcription factors.1 THZ1 is reported to induce apoptotic cell death in triple-negative breast cancer cells that are highly dependent on Cdk7.2
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1. Kwiatkowski, N., Zhang, T., Rahl, P.B., et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor Nature 511(7511), 616-620 (2014).
Wang, Y., Zhang, T., Kwiatkowski, N., et al. CDK7-