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Nifuroxazide STAT inhibitor

Name: Nifuroxazide
Brand: Selleck Chemicals
SKU: S4182
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S4182

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.

Chemical Structure

Molecular Weight: 275.22

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	EGFR JAK Pim
Other STAT Inhibitors	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 HO-3867 Homoharringtonine (HHT)

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (199.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (2.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	275.22	Formula	C₁₂H₉N₃O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	965-52-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC=C1C(=O)NN=CC2=CC=C(O2)[N+](=O)[O-])O

Mechanism of Action

Targets/IC₅₀/Ki	STAT1 STAT3 STAT5
In vitro	Nifuroxazide is a nitrofuran compound inhibitor of STAT transcription factor signaling. This compound 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. It 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 this chemical for Jak2 and Tyk2. It shows no inhibition of Akt or MAPK phosphorylation. This inhibitor 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. It 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, this compound can overcome this survival advantage. Reflecting the interaction of STAT3 with other cellular pathways, it shows enhanced cytotoxicity when combined with either the histone deacetylase inhibitor depsipeptide or the MEK inhibitor UO126.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18824601/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		26830149
Western blot	p-STAT3 / STAT3 / p-FAK / FAK / p-Src / Src MMP-9 / MMP-2		26830149

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05754996	Recruiting	Hepatic Encephalopathy	Cairo University	March 12 2023	Phase 3

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Handling Instructions

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