THZ1THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.
IC50 value: 3.2 nM (Kd for CDK7)[1]
Target: CDK7
THZ1 has the unprecedented ability to target a remotecysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
Cancer cell-line profiling indicates that a subset of cancer cell lines,
including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1.
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