Caspase-3 inhibitor,selective non-peptide
| Cas No. | 331645-84-2 |
| 化学名 | 2-(3,4-dichloroanilino)-6-nitro-4-oxo-N-prop-2-enyl-1H-quinazoline-8-carboxamide |
| Canonical SMILES | C=CCNC(=O)C1=C2C(=CC(=C1)[N+](=O)[O-])C(=O)N=C(N2)NC3=CC(=C(C=C3)Cl)Cl |
| 分子式 | C18H13Cl2N5O4 |
| 分子量 | 434.23 |
| 溶解度 | <10.86mg/ml in DMSO |
| 储存条件 | Store at RT |
| 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 | AZ 10417808 is a selective caspase-3 inhibitor with IC50 value of 14.9 uM [1].
The caspase-3 protein is a member of the cysteine-aspartic acid protease (caspase) family. Sequential activation of caspases plays a central role in the execution-phase of cell apoptosis [1].
AZ 10417808 (AQZ-1) is a potent small molecule nonpeptidic inhibitor of caspase-3, which block cellular and biochemical features of apoptosis [1].
AZ 10417808 was evaluated for its inhibitory activity against caspases 1, 2, 3, 6, 7, 8 and only caspases-3 was potently inhibited. AZ 10417808 completely blocked the staurosporine-induced intracellular DEVDase activity and this effect was dose-dependent. Of control cells ( 64 ± 7%) whereas cells treated with staurosporine plus 10 μM AZ 10417808 had 92 ± 2% viability, which indicated that the AZ 10417808 enhanced cell viability in SH-SY5Y cell culture apoptosis paradigm [1].
Reference:
[1]. Scott CW, Briner CS, Wilkins DE, et al. Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis. J Pharmacol Exp Ther, 2003, 304(1): 433-40. |
