NS3694

- Overview
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    Background
    
    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.
- Properties
  - Alternative Name
    
    Apoptosis Inhibitor II; 4-chloro-2-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzoic acid
    
    CAS Number
    
    426834-38-0
    
    Molecular Formula
    
    C15H10ClF3N2O3
    
    Molecular Weight
    
    358.7
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤14mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Barot S, Abo-Ali EM, et al. "Inhibition of glycogen catabolism induces intrinsic apoptosis and augments multikinase inhibitors in hepatocellular carcinoma cells." Exp Cell Res. 2019 Aug 15;381(2):288-300. PMID:31128107

NS3694

Background

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