NIK-IN-3
NIK-IN-3 is a potent and orally active NF-κB-inducing kinase (NIK) inhibitor with an IC50 of 5.2 nM. NIK-IN-3 suppresses non-canonical NF-κB pathway activation and inhibits the secretion of pro-inflammatory cytokines, such as TNF-α, IL-6, IL-1β and chemokine CXCL12. NIK-IN-3 shows significant anti-inflammatory effects in LPS (HY-D1056)-induced sepsis mice model and DSS (HY-116282)-induced colitis model. NIK-IN-3 can be used for the research of inflammation, such as colitis.
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- 화학식: C26H24ClN7O2S
- 분자량:534.03
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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NF-κB 5.2 nM (IC50) |
IL-6 |
IL-1β |
NIK-IN-3 (Compound 38) (1-5 μM) effectively suppresses non-canonical NF-κB pathway activation in HEK293 cells[1].
NIK-IN-3 (100 nM; 3 days) suppresses Th17 cell differentiation in murine naive CD4+ T cells with no notable cytotoxicity[1].
NIK-IN-3 (5 μM; 22 h) inhibits the secretion of pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) and chemokine CXCL12 in LPS (HY-D1056)+CD40-induced RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | Cmax | T1/2 | CL | C0 | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 1.0 mg/kg | i.v. | 428.27 ng·h/mL | 978.27 ng/mL | 0.83 h | 39.23 mL/min/kg | 1421.23 ng/mL | / | / |
| Mice | 10 mg/kg | p.o. | 1923.05 ng·h/mL | 1364.03 ng/mL | 1.08 h | / | / | 0.42 h | 45.0 % |
NIK-IN-3 (25-50 mg/kg, p.o., daily for 7 days) ameliorates colitis symptoms in C57BL/6 mice (DSS (HY-116282C)-induced colitis model)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (DSS-induced colitis model)[1]
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Dosage:25 mg/kg, 50 mg/kg
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Administration:Orally administration
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Result:Ameliorated the DSS-induced colitis model, reducing disease activity index (DAI) and body weight loss.
Preserved colon length and reduced histopathological damage, including epithelial erosion, crypt architecture loss, and inflammatory cell infiltration. Upregulated the precursor protein p100 and reduced the active form p52, indicating suppression of the non-canonical NF-κB pathway.
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Animal Model:C57BL/6 mice (LPS-induced sepsis model)[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneally injection
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Result:Improved survival in the LPS-induced sepsis model, with a 30% survival rate at 7 days.
Reduced serum levels of pro-inflammatory cytokines (IFN-γ, TNF-α, IL-1β, IL-6, CXCL12) and protected against liver injury, as evidenced by reduced ALT and AST levels. Reduced necrotic foci and macrophage infiltration.
Chemical Information
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분자량 534.03
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화학식 C26H24ClN7O2S
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SMILES
ClC1=CC(NC2=NC=CC(NC3=CC(C#C[C@](O)(C)C4=NC=CS4)=CC=C3N5CCOCC5)=N2)=NC=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NIK-IN-3 Related Classifications
HY-179701 Related Classifications
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