Nifuroxazide

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.

Nifuroxazide Chemical Structure

Nifuroxazide Chemical Structure

CAS No. 965-52-6

Purity & Quality Control

Nifuroxazide Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U3A cells Function assay 1 h Inhibition of STAT3 expressed in human U3A cells after 1 hr by luciferase reporter gene assay, EC50=3 μM 22650325
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Biological Activity

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.
Targets
STAT1 [1] STAT3 [1] STAT5 [1]
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot MMP-9 / MMP-2 p-STAT3 / STAT3 / p-FAK / FAK / p-Src / Src 28055016
Growth inhibition assay Cell viability 26830149
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05754996 Recruiting
Hepatic Encephalopathy
Cairo University
March 12 2023 Phase 3

Chemical Information & Solubility

Molecular Weight 275.22 Formula

C12H9N3O5

CAS No. 965-52-6 SDF Download Nifuroxazide SDF
Smiles C1=CC(=CC=C1C(=O)NN=CC2=CC=C(O2)[N+](=O)[O-])O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 55 mg/mL ( (199.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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