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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C26H24ClN7O2S
- 分子量:534.03
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
NF-κB 5.2 nM (IC50) |
IL-6 |
IL-1β |
体外実験
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.
Parmacokinetics
| 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 % |
体内実験
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.
化学情報
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分子量 534.03
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NIK-IN-3 関連分類
HY-179701 関連分類
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