Identification | Back Directory | [Name]
NS 3694 | [CAS]
426834-38-0 | [Synonyms]
Apoptosis Inhibitor II, NS3694 Apoptosis Inhibitor II, NS3694 - CAS 426834-38-0 - Calbiochem Benzoic acid, 4-chloro-2-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]- | [Molecular Formula]
C15H10ClF3N2O3 | [MDL Number]
MFCD00249000 | [MOL File]
426834-38-0.mol | [Molecular Weight]
358.7 |
Hazard Information | Back Directory | [Description]
Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome. NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation. It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 μM. NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1. It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine . NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death. | [Uses]
NS3694 is a suppressor of the formation of apoptosome Apaf-1. | [Definition]
ChEBI: 4-chloro-2-[[oxo-[3-(trifluoromethyl)anilino]methyl]amino]benzoic acid is a member of ureas. | [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]. | [IC 50]
approximately 50 μm for cytochrome c-induced caspase activation in hela cell cytosolic extracts | [References]
[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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Energy Chemical
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InvivoChem
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Creative Enzymes
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