Description | THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively. |
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Targets | CDK13 [1]() | CDK12 [1]() | 69 nM | 158 nM |
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In vitro | THZ531 treatment leads to a dramatic and irreversible decrease in Jurkat cell proliferation with an IC50 of 50 nM. THZ531 induces apoptosis in a dose- and time-dependent manner with low doses (<350 nM) leading to slow onset of apoptosis over several cell doublings, while doses exceeding 350 nM induce rapid apoptosis which may result from a combination of on- and off- target effects. THZ531 reduces Pol II CTD Ser2 phosphorylation (pSer2) in a concentration-dependent manner[1]. |
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