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

NIK-IN-3 是一种强效且具有口服活性的 NF-κB 诱导激酶 (NIK) 抑制剂，其 IC50 值为 5.2 nM。NIK-IN-3 可抑制非经典 NF-κB 通路的激活，并能抑制促炎细胞因子，如 TNF-α、IL-6、IL-1β 和趋化因子 CXCL12 的分泌。NIK-IN-3 在 LPS (HY-D1056) 诱导的脓毒症小鼠模型以及 DSS (HY-116282C) 诱导的结肠炎模型中显示出显著的抗炎效果。NIK-IN-3 可用于炎症相关研究，如结肠炎。

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NIK-IN-3

NIK-IN-3 Chemical Structure

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NIK-IN-3 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

查看 CXCR 亚型特异性产品:

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

NIK-IN-3 (Compound 38) (1-5 μM) 在 HEK293 细胞中有效抑制非经典 NF-κB 通路的激活[1]。
NIK-IN-3 (100 nM; 3 天) 在小鼠原始 CD4+ T 细胞中抑制 Th17 细胞分化，且无明显细胞毒性[1]。
NIK-IN-3 (5 μM; 22 小时) 抑制 LPS (HY-D1056) 和 CD40 诱导的 RAW264.7 细胞分泌 TNF-α、IL-6、IL-1β 及 CXCL12 等炎症因子[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NIK-IN-3 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice 1.0 mg/kg i.v. AUC0-∞ 428.27 ng·h/mL
Mice 1.0 mg/kg i.v. Cmax 978.27 ng/mL
Mice 1.0 mg/kg i.v. T1/2 0.83 h
Mice 1.0 mg/kg i.v. CL 39.23 mL/min/kg
Mice 1.0 mg/kg i.v. C0 1421.23 ng/mL
Mice 10 mg/kg p.o. AUC0-∞ 1923.05 ng·h/mL
Mice 10 mg/kg p.o. Cmax 1364.03 ng/mL
Mice 10 mg/kg p.o. T1/2 1.08 h
Mice 10 mg/kg p.o. Tmax 0.42 h
Mice 10 mg/kg p.o. F 45.0 %
体内研究
(In Vivo)

NIK-IN-3 (Compound 38) (10 mg/kg，腹腔注射) 通过抑制非经典 NF-κB 通路， 可改善 LPS (HY-D1056) 诱导的败血症模型小鼠的生存率并减少炎症 [1] 。
NIK-IN-3 (25-50 mg/kg，口服，每日 1 次，连续 7 天) 在 C57BL/6 小鼠 (DSS (HY-116282C) 诱导的结肠炎模型) 中改善 C57BL/6 小鼠的结肠炎症状[1] 。

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.
分子量

534.03

Formula

C26H24ClN7O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NIK-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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