AZ 10417808
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.
- 1. Jesse R Poganik, Kuan-Ting Huang, et al. "Wdr1 and cofilin are necessary mediators of immune-cell-specific apoptosis triggered by Tecfidera." Nat Commun. 2021 Sep 30;12(1):5736. PMID: 34593792
- 2. Chang-Yong Choi, Mai Tram Vo, et al. "Autophagy-competent mitochondrial translation elongation factor TUFM inhibits caspase-8-mediated apoptosis." Cell Death Differ. 2022 Feb;29(2):451-464. PMID: 34511600
- 3. Jiao C, Chen W, et al. "Ganoderma lucidum spore oil induces apoptosis of breast cancer cells in vitro and in vivo by activating caspase-3 and caspase-9." J Ethnopharmacol. 2019 Oct 3:112256. PMID: 31586690
| Physical Appearance | Yellow solid |
| Storage | Store at RT |
| M.Wt | 434.23 |
| Cas No. | 331645-84-2 |
| Formula | C18H13Cl2N5O4 |
| Solubility | <10.86mg/ml in DMSO |
| Chemical Name | 2-(3,4-dichloroanilino)-6-nitro-4-oxo-N-prop-2-enyl-1H-quinazoline-8-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | C=CCNC(=O)C1=C2C(=CC(=C1)[N+](=O)[O-])C(=O)N=C(N2)NC3=CC(=C(C=C3)Cl)Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
