NF-κB/STAT3/iNOS-IN-1
NF-κB/STAT3/iNOS-IN-1 is a NF-κB/STAT3/iNOS inhibitor. NF-κB/STAT3/iNOS-IN-1 reduces the expression of inflammatory mediators TNF-α, IL-1β, IL-6, IL-8 and COX-2. NF-κB/STAT3/iNOS-IN-1 upregulates the expression of epithelial barrier-related proteins E-cadherin, Occludin and Zonula occludens-1. NF-κB/STAT3/iNOS-IN-1 alleviates disease severity and histopathological damage in mouse colitis models. NF-κB/STAT3/iNOS-IN-1 can be used for the research of inflammatory bowel disease (colitis).
For research use only. We do not sell to patients.
- Formula: C24H21N3O5
- Molecular Weight:431.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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STAT3 |
iNOS |
IL-1β |
IL-6 |
IL-8 |
COX-2 |
NF-κB/STAT3/iNOS-IN-1 (Compound 10E) (3 μM; 30 min pre-incubation) potently inhibits LPS-induced nitrite production in RAW 264.7 murine macrophages, and preliminary screening shows that it achieves the maximum inhibitory effect at 3 μM[1].
NF-κB/STAT3/iNOS-IN-1 (1-10 μM) dose-dependently inhibits LPS-induced nuclear translocation of NF-κB and p-STAT3, and reduces the expression of pro-inflammatory mediators including iNOS, TNF-α, IL-1β, IL-6 and IL-8 in RAW 264.7 mouse macrophages[1].
NF-κB/STAT3/iNOS-IN-1 (1 μM; 1 h) potently inhibits TNF-α-induced adhesion of U937 monocytes to HT-29 colonic epithelial cells[1].
NF-κB/STAT3/iNOS-IN-1 (0.1-100 μM; 48 h) exhibits only extremely low cytotoxicity in RAW 264.7 mouse macrophages and HT-29 colon epithelial cells[1].
NF-κB/STAT3/iNOS-IN-1 (1-10 μM) dose-dependently inhibits TNF-α-induced nuclear translocation of NF-κB and p-STAT3, reduces the expression of pro-inflammatory mediators, and upregulates the expression of epithelial barrier-related proteins in human colonic epithelial cells HT-29[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 murine macrophages, HT-29 human colonic epithelial cells
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Concentration:10 μM; 0.1-100 μM
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Incubation Time:48 h
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Result:Showed minimal cytotoxicity in both cell lines at 10 μM, with viability comparable to vehicle-treated controls.
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Cell Line:LPS-stimulated RAW 264.7 murine macrophages
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Concentration:1-10 μM
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Incubation Time:pre-incubation followed by LPS stimulation
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Result:Dose-dependently blocked LPS-induced nuclear translocation of NF-κB in RAW 264.7 cells.
Dose-dependently reduced nuclear accumulation of phosphorylated STAT3 (p-STAT3) in RAW 264.7 cells.
Dose-dependently reduced total protein levels of iNOS, TNF-α, IL-1β, IL-6, and IL-8 relative to LPS-only treated cells.
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Cell Line:TNF-α-stimulated HT-29 human colonic epithelial cells
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Concentration:1-10 μM
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Incubation Time:pre-incubation followed by TNF-α stimulation
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Result:Dose-dependently attenuated TNF-α-induced nuclear accumulation of NF-κB in HT-29 cells.
Dose-dependently attenuated TNF-α-induced nuclear accumulation of p-STAT3 in HT-29 cells.
Dose-dependently reduced total protein levels of iNOS, COX-2, TNF-α, IL-1β, IL-6, and IL-8 relative to TNF-α-only treated cells.
Dose-dependently increased total protein levels of epithelial barrier-associated proteins E-cadherin, occludin, and zonula occludens-1 (ZO-1) relative to TNF-α-only treated cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 N/Crl (female, 6 weeks old, DSS-induced colitis)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Ameliorated DSS-induced body weight loss and reduced disease activity index (DAI) scores in a dose-dependent manner.
Attenuated colonic shortening and reduced colon weight per unit length at 10 mg/kg.
Significantly suppressed DSS-induced elevation of colonic MPO levels at both doses.
Reduced mucosal damage, inflammatory cell infiltration, and crypt distortion, lowering histopathological scores in a dose-dependent manner.
Inhibited DSS-induced nuclear translocation of NF-κB and phosphorylated STAT3 (p-STAT3) in colonic tissue in a dose-dependent manner.
Suppressed the expression of inflammatory mediators including iNOS, COX-2, TNF-α, IL-1β, IL-6, and IL-8 in a dose-dependent manner.
Increased the expression of the epithelial barrier protein E-cadherin in a dose-dependent manner.
Chemical Information
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Molecular Weight 431.44
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Formula C24H21N3O5
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SMILES
COC([C@H](CC1=CC=C(C(O)=C1)O)NC(C2=C(N=C3N2C=CC=C3)C4=CC=CC=C4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NF-κB/STAT3/iNOS-IN-1 Related Classifications
HY-184692 Related Classifications
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