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Formula | C12H9N3O5 |
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Molecular Weight | 275.22 | CAS No. | 965-52-6 | |
Solubility (25°C)* | In vitro | DMSO | 55 mg/mL (199.84 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Nifuroxazide is a cell-permeable and orally available 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. | |||
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Targets |
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In vitro | 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. [1] |
Data from [Data independently produced by , , PLoS One, 2017, 12(2):e0172178]
Data from [Data independently produced by , , Onco Targets Ther, 2017, 10:1767-1776]
Glucocorticoid activates STAT3 and NF-κB synergistically with inflammatory cytokines to enhance the anti-inflammatory factor TSG6 expression in mesenchymal stem/stromal cells [ Cell Death Dis, 2024, 15(1):70] | PubMed: 38238297 |
Induced expression modes of genes related to Toll, Imd, and JAK/STAT signaling pathway-mediated immune response in Spodoptera frugiperda infected with Beauveria bassiana [ Front Physiol, 2023, 14:1249662] | PubMed: 37693000 |
Induced expression modes of genes related to Toll, Imd, and JAK/STAT signaling pathway-mediated immune response in Spodoptera frugiperda infected with Beauveria bassiana [ Front Physiol, 2023, 10.3389/fphys.2023.1249662] | PubMed: 37693000 |
A functional variant of CD40 modulates clearance of hepatitis B virus in hepatocytes via regulation of the ANXA2/CD40/BST2 axis [ Hum Mol Genet, 2023, 32(8):1334-1347] | PubMed: 36383401 |
Nifuroxazide induces the apoptosis of human non‑small cell lung cancer cells through the endoplasmic reticulum stress PERK signaling pathway [ Oncol Lett, 2023, 25(6):248] | PubMed: 37153034 |
Tumor-derived lactate inhibit the efficacy of lenvatinib through regulating PD-L1 expression on neutrophil in hepatocellular carcinoma [ J Immunother Cancer, 2021, 9(6)e002305] | PubMed: 34168004 |
Inhibition of Dot1L Alleviates Fulminant Hepatitis through Myeloid Derived Suppressor Cells [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9] | PubMed: 33497867 |
Препараты Нифуроксазида в Российской Федерации. Сообщение первое: номенклатура и химико-фармацевтические характеристики состава [ Antibiotics and chemotherapy, 2021, 66: 7–8: 90–98.] | PubMed: none |
[ Signal Transduct Target Ther, 2020, ] | PubMed: 32855386 |
Inflammation-induced inhibition of chaperone-mediated autophagy maintains the immunosuppressive function of murine mesenchymal stromal cells. [ Cell Mol Immunol, 2020, 10.1038/s41423-019-0345-7] | PubMed: 31900460 |
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