thz1 dihydrochloride

THZ1 2HCl (THZ1 Dihydrochloride) is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.

THZ1 Hydrochloride is a potent, selective covalent inhibitor of CDK7, exhibiting an IC50 value of 3.2 nM. It also targets closely related kinases CDK12 and CDK13, leading to the downregulation of MYC expression.

THZ1-R is a non-covalent active analogue of THZ1, with the acrylamide group removed from THZ1, losing its ability to covalently bind to the C312 cysteine residue of CDK7. Its CDK7 inhibitory activity is weaker than that of THZ1.

THZ1 (CDK7 inhibitor) is a selective covalent inhibitor of CDK7, exhibiting binding affinity to the cysteine residue located at the outer end of the classical kinase domain, thus conferring high selectivity for CDK7, with an IC50 of 3.2 nM.