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    Nifuroxazide
    Nifuroxazide

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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 #: V1382
    CAS #: 965-52-6Purity ≥98%

    Description: Nifuroxazide (Bacifurane; Diafuryl; Ambatrol; Antinal; Diarlidan) is a potent, cell-permeable and orally bioavailable nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells. It is a nitrofuran antibiotic that has been approved for treating colitis and diarrhea. Nifuroxazide is described to block constitutive phosphorylation of STAT3 by reducing Jak kinase autophosphorylation, decreasing the viability of myeloma cells depending on constitutive STAT3 activity for survival while not affecting normal peripheral blood mononuclear cells.

    References: Blood. 2008 Dec 15;112(13):5095-102.

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    Molecular Weight (MW)275.22
    FormulaC12H9N3O5
    CAS No.965-52-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 55 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 4-Hydroxy-N-[(E)-(5-nitrofuran-2-yl)methylideneamino]benzamide

    InChi Key: YCWSUKQGVSGXJO-NTUHNPAUSA-N

    InChi Code: InChI=1S/C12H9N3O5/c16-9-3-1-8(2-4-9)12(17)14-13-7-10-5-6-11(20-10)15(18)19/h1-7,16H,(H,14,17)/b13-7+

    SMILES Code: O=C(N/N=C/C1=CC=C([N+]([O-])=O)O1)C2=CC=C(O)C=C2           

    Synonyms

    Nifuroxazide; Bacifurane; Diafuryl; Ambatrol; Antinal; Diarlidan


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    In Vitro

    In vitro activity: Nifuroxazide is a nitrofuran compound inhibitor of STAT transcription factor signaling. Nifuroxazide is described to block constitutive phosphorylation of STAT3 by reducing Jak kinase autophosphorylation, decreasing the viability of myeloma cells depending on constitutive STAT3 activity for survival while not affecting normal peripheral blood mononuclear cells. Nifuroxazide produces decreases in tyrosine phosphorylation of Jak2 and Tyk2, and showed no effects on EGF receptor tyrosine kinase or Src kinase, indicating a relative specificity of Nifuroxazide for Jak2 and Tyk2. Nifuroxazide shows no inhibition of Akt or MAPK phosphorylation. Nifuroxazide inhibits the constitutive phosphorylation of STAT3 in MM cells by reducing Jak kinase autophosphorylation, and leads to down-regulation of the STAT3 target gene Mcl-1. Nifuroxazide causes a decrease in viability of primary myeloma cells and myeloma cell lines containing STAT3 activation, but not normal peripheral blood mononuclear cells. Although bone marrow stromal cells provide survival signals to myeloma cells, nifuroxazide can overcome this survival advantage. Reflecting the interaction of STAT3 with other cellular pathways, nifuroxazide shows enhanced cytotoxicity when combined with either the histone deacetylase inhibitor depsipeptide or the MEK inhibitor UO126.

    In VivoCompared with the vehicle group, treatment with Nifuroxazide could inhibit tumor growth and tumor weight in a dose-dependent manner, with the inhibition rate of tumor volumes being 43.0% and 62.1% at 25 mg/kg and 50 mg/kg, respectively. It is also shown that Nifuroxazide significantly inhibits the proliferation of nuclear Ki-67-positive cells and induces apoptosis cells of cleaved caspase-3-positive cells. Besides, it is found that treatment with Nifuroxazide could inhibit the expression of MMP-2, MMP-9 and p-Stat3 in A375 tumor tissues. What’s more, Nifuroxazide inhibits the infiltration of MDSCs into the lung, which might be associated with suppression of distant colonization of tumor cells in B16-F10 melanoma metastasis model.
    Animal modelMice
    Formulation & Dosage25 mg/kg, 50 mg/kg; i.p.
    References

    Blood. 2008 Dec 15;112(13):5095-102. doi


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

    Nifuroxazide

    Nifuroxazide inhibits the viability of MM cells containing constitutive STAT3 phosphorylation. Blood. 2008 Dec 15;112(13):5095-102.
     

    Nifuroxazide

    Nifuroxazide inhibits STAT3, Jak2, and Tyk2 tyrosine phosphorylation. Blood. 2008 Dec 15;112(13):5095-102.
     

    Nifuroxazide

    Nifuroxazide inhibits the viability of MM cells containing constitutive STAT3 phosphorylation. Blood. 2008 Dec 15;112(13):5095-102.


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