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A non-cysteine reactive derivative of THZ1
THZ1-R is a non-cysteine reactive derivative of the cyclin-dependent kinase 7 (Cdk7) inhibitor THZ1 .1 THZ1-R inhibits Cdk7 (IC50s = 142-241 nM) less potently than THZ1 and lacks antiproliferative activity against T cell acute lymphoblastic leukemia (T-ALL) cell lines.
1.Kwiatkowski, N., Zhang, T., Rahl, P.B., et al.Targeting transcription regulation in cancer with a covalent CDK7 inhibitorNature511(7511)616-620(2014)
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