NS3694
Catalogue Number: C4468-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C15H10ClF3N2O3 |
| Physical state: | A crystalline solid |
| Type: | Other Inhibitors |
| Alias: | Apoptosis Inhibitor II |
| Shipping Condition: | Blue Ice |
| Unit(s): | 10 mg, 25 mg, 5 mg, 50 mg |
Description
Description: IC50: approximately 50 µM for cytochrome c-induced caspase activation in HeLa cell cytosolic extracts NS3694 inhibits apoptosome formation and caspase activation. The release of mitochondrial proapoptotic proteins into the cytosol is a critical event in apoptosis signaling, resulting in the activation of caspases. Once in the cytosol, cytochrome c triggers the formation of a caspase-activating protein complex called the apoptosome, while Smac/Diablo and Omi/htra2 antagonize the caspase inhibitory effect.In vitro: Previous study found that NS3694, and its two analogs (NS1764 and NS1784) were well-tolerated by MCF-7S1 breast cancer cells at concentrations up to 100, 50, and 25 µM, respectively. Moreove, all three compounds could not inhibit recombinant caspase 9 and caspase 3 at concentrations ranging from 25 to 100 µM. In addition, NS3694 was able to inhibit the co-immunoprecipitation of caspase 9 and Apaf-1 from HeLa cell cytosol stimulated by cytochrome c and dATP. NS3694 could also inhibit the formation of the active 700-kDa apoptosome complex, but had no effect on TNF-induced caspase-independent death of WEHI-S cells. NS3694 did not inhibit FasL-induced caspase activation or death in type I cells neither [1].In vivo: Up to now, there is no animal in vivo study reported.Clinical trial: So far, no clinical study has been conducted.Reference:[1] Lademann, U.,Cain, K.,Gyrd-Hansen, M., et al. Diarylurea compounds inhibit caspase activation by preventing the formation of the active 700-kilodalton apoptosome complex. Mol.Cell Biol. 23(21), 7829-7837 (2003).
Additional Text
Storage Note
Store at -20°C
Smile String
ClC1=CC=C(C(O)=O)C(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C1
Solubility
≥46 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
C4468 CofA
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