CAS NO: | 331645-84-2 |
包装: | 5mg |
规格: | 98% |
市场价: | 3254元 |
分子量: | 434.23 |
Background:
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.