Nifuroxazide

Catalog No.S4182

For research use only.

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

CAS No. 965-52-6

Selleck's Nifuroxazide has been cited by 15 publications

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U3A cells NE\yOWNHfW6ldHnvckBie3OjeR?= NXm4Wm5JOSCq NHnLSY9KdmirYnn0bY9vKG:oIGPURXQ{KGW6cILld5Nm\CCrbjDoeY1idiCXM1GgZ4VtdHNiYX\0[ZIhOSCqcjDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OyEQvF2= NYHic2NyOjJ4NUCzNlU>
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 26830149
Western blot p-STAT3 / STAT3 / p-FAK / FAK / p-Src / Src ; MMP-9 / MMP-2 26830149 28055016

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 275.22
Formula

C12H9N3O5

CAS No. 965-52-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC=C1C(=O)NN=CC2=CC=C(O2)[N+](=O)[O-])O

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