2. NF-κB Apoptosis Immunology/Inflammation GPCR/G Protein
  3. NF-κB TNF Receptor Interleukin Related CXCR
  4. 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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NIK-IN-3

NIK-IN-3 Chemical Structure

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NIK-IN-3 Related Antibodies

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Description

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[1].

IC50 & Target[1]

NF-κB

5.2 nM (IC50)

IL-6

 

IL-1β

 

In Vitro

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.

NIK-IN-3 Related Antibodies
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 %
In Vivo

NIK-IN-3 (Compound 38) (10 mg/kg, i.p., single dose) improves survival and reduces inflammation in an LPS (HY-D1056)-induced sepsis mice model by inhibiting the non-canonical NF-κB pathway[1].
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.

Animal Model: C57BL/6 mice (DSS-induced colitis model)[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Orally administration
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.
Animal Model: C57BL/6 mice (LPS-induced sepsis model)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneally injection
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.
Molecular Weight

534.03

Formula

C26H24ClN7O2S
SMILES

ClC1=CC(NC2=NC=CC(NC3=CC(C#C[C@](O)(C)C4=NC=CS4)=CC=C3N5CCOCC5)=N2)=NC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NIK-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NIK-IN-3NF-κBTNF ReceptorInterleukin RelatedCXCRNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILCXC chemokine receptorsC-X-C motif chemokine receptorsSepsisHEK293Th17CD40P100P52Inhibitorinhibitorinhibit

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