DESCRIPTION
THZ1 is a covalent inhibitor of CDK7 with IC50 value of 3.2nM [1]. 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 [1].
| CAS NO | 19608-29-10 |
|---|---|
| Synonym Name | THZ1Covalent CDK7 |
| Chemical Name | (E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide |
| Chemical Formula | C31H28ClN7O2 |
| Molecular Weight | 566.05 |
| Sequence | ClC1=CN=C(N=C1C2=CNC3=CC=CC=C23)NC4=CC=CC(NC(C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5)=O)=C4 |
| Appearance | NA |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| Disclaimer | For research purposes only. Not suitable for human or animal care nor for in-vivo or diagnostic use. |
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