THZ1-R

Description: THZ1-R is a novel and non-cysteine reactive analog of THZ1 which shows lower activity for CDK7 inhibition with a Kd of 142 nM for binding to CDK7. THZ1 is a novel, potent, selective and covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. THZ1 covalently modifies CDK7 by targeting C312 residue outside of the kinase domain, providing an unanticipated means of achieving covalent selectivity. THZ1 potently inhibits proliferation of Jurkat and Loucy T-ALL cell lines with IC50 values of 50nM and 0.55nM, respectively. In the kinase binding assay, THZ1 shows a good binding affinity with IC50 value of 3.2nM.

References: Nature. 2014 Jul 31; 511(7511):616-20; Mol Cell. 2015 Aug 20; 59(4):576-87

Relatated CAS: 1604810-83-4 (THZ1 free); 1604811-14-4 (bio-THZ1, biotinylated THZ1); 1621523-07-6 (THZ1-R, the non-cysteine reactive analog of THZ1)