Potent and selective ATP-competitive inhibitor of Chk1 and Chk2; also enhances CRISPR-Cpf1-mediated genome editing
| Cas No. | 1246094-78-9 |
| Canonical SMILES | FC1=CC=CC(C2=CC(NC(N)=O)=C(C(N[C@@H]3CNCCC3)=O)S2)=C1.Cl |
| 分子式 | C17H19FN4O2S.HCl |
| 分子量 | 398.88 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50 vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents. Active in vivo. Also improves efficiency of CRISPR-Cpf1-mediated genome editing in hPSC lines (2.7-fold at 1 μM). Zabludoff et al (2008) AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol. Cancer Ther. 7 2955 PMID:18790776 |Morgan et al (2010) Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Res. 70 4972 PMID:20501833 |Ma et al (2018) Small molecules promote CRISPR-Cpf1-mediated genome editing in human pluripotent stem cells. Nat Commun. 9 1303 PMID:29610531 |
