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NS3694
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NS3694图片
CAS NO:426834-38-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
NS3694 是一种二芳基脲化合物,是一种凋亡体抑制剂。 NS3694 抑制凋亡小体形成和半胱天冬酶活化。
Cas No.426834-38-0
别名Apoptosis Inhibitor II
化学名4-chloro-2-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzoic acid
Canonical SMILESClC1=CC=C(C(O)=O)C(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C1
分子式C15H10ClF3N2O3
分子量358.7
溶解度≤14mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).