THZ1 - Covalent CDK7 Inhibitor. CAS# 1604810-83-4 284 Smiles: C(NC1N=CC=CN=1)C1C=CC(CNC2N=CC=CN=2)=CC=1

Smiles: C(NC1N=CC=CN=1)C1C=CC(CNC2N=CC=CN=2)=CC=1

Dominguez E

110 nM and 70 nM

disrupts YAP-TEAD interactions and enhances trypsin cleavage of YAP with EC50 ~100 nM

513(7516):124-7

THZ1 - Covalent CDK7 Inhibitor. CAS# 1604810-83-4 284 Smiles: C(NC1N=CC=CN=1)C1C=CC(CNC2N=CC=CN=2)=CC=1THZ1, CAS No. 1604810 83 4, is a novel potent, selective and cell permeable irreversible CDK7 inhibitor with an IC50 ~3. 2 nM. THZ1 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. Cancer cell line profiling indicates that a subset of cancer cell lines, including human T cell acute lymphoblastic leukaemia (T ALL), have