| CAS NO: | 426834-38-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 358.7 |
| Cas No. | 426834-38-0 |
| Formula | C15H10ClF3N2O3 |
| Synonyms | Apoptosis Inhibitor II |
| Solubility | ≤14mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide |
| Chemical Name | 4-chloro-2-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzoic acid |
| Canonical SMILES | ClC1=CC=C(C(O)=O)C(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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).
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