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    Necrosulfonamide
    Necrosulfonamide

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V2915
    CAS #: 1360614-48-7Purity ≥98%

    Description: Necrosulfonamide is a potent and highly specific and potent necrosis inhibitor which blocks mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. Necrosulfonamide has no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells, even at 5 μM concentration. The receptor-interacting serine-threonine kinase 3 (RIP3) is a key signaling molecule in the programmed necrosis (necroptosis) pathway. This pathway plays important roles in a variety of physiological and pathological conditions, including development, tissue damage response, and antiviral immunity. 

    References:  2012 Jan 20;148(1-2):213-27. 


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    Molecular Weight (MW)461.47 
    FormulaC18H15N5O6S2
    CAS No.1360614-48-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 92 mg/mL (199.36 mM)
    Water: <1 mg/mL
    Ethanol: N/A
    SMILES Code O=C(NC1=CC=C(S(=O)(NC2=NC=CN=C2OC)=O)C=C1)/C=C/C3=CC=C([N+]([O-])=O)S3
    Synonyms Necrosulfonamide; N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide; (E)-Necrosulfonamide 


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    In Vitro

    In vitro activity: Necrosulfonamide is a potent and highly specific and potent necrosis inhibitor which blocks mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. Necrosulfonamide has no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells, even at 5 μM concentration. The receptor-interacting serine-threonine kinase 3 (RIP3) is a key signaling molecule in the programmed necrosis (necroptosis) pathway. This pathway plays important roles in a variety of physiological and pathological conditions, including development, tissue damage response, and antiviral immunity.   


    Kinase Assay: RIP1 and RIP3 were immunoprecipitated with an anti-Flag antibody. The Flag beads were washed three times with kinase buffer (50 mM HEPES, pH 7.5, 10 mM MgCl2, 50 mM NaCl, 0.02% BSA, 150 μM ATP and 1 mM DTT), then incubated with 2 μCi of [32P]γ-ATP at 37°C for 1 hour with the artificial substrate MBP or purified recombinant MLKL. The reaction mixtures were then subjected to SDS-PAGE followed by autoradiography. we report the identification of a small molecule called (E)-N-(4-(N-(3-methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide--hereafter referred to as necrosulfonamide--that specifically blocks necrosis downstream of RIP3 activation. An affinity probe derived from necrosulfonamide and coimmunoprecipitation using anti-RIP3 antibodies both identified the mixed lineage kinase domain-like protein (MLKL) as the interacting target. MLKL was phosphorylated by RIP3 at the threonine 357 and serine 358 residues, and these phosphorylation events were critical for necrosis.


    Cell Assay: Treating cells with necrosulfonamide or knocking down MLKL expression arrested necrosis at a specific step at which RIP3 formed discrete punctae in cells.

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    References  2012 Jan 20;148(1-2):213-27.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Necrosulfonamide

    Necrosulfonamide Blocks Necrosis Downstream of RIP3 Activation.  2012 Jan 20;148(1-2):213-27.

     

    Necrosulfonamide

    Necrosulfonamide Specifically Inhibits Necrosis in Multiple Human Cell Lines.  2012 Jan 20;148(1-2):213-27.

     

    Necrosulfonamide

    Identification of Cellular Targets of Necrosulfonamide.  2012 Jan 20;148(1-2):213-27.


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