2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. NF-κB Keap1-Nrf2 Heme Oxygenase (HO) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) SOD
  4. NF-κB-IN-20

NF-κB-IN-20 是一种口服有效的 NF-κB 抑制剂。NF-κB-IN-20 会直接与 Keap1 蛋白结合，激活 Keap1/Nrf2/HO-1 抗氧化途径，同时抑制 NF-κB 炎症途径，从而协同降低氧化应激和炎症反应。NF-κB-IN-20 M11 可抑制 IL-6、IL-1β 和 TNF-α 的表达，显著降低 ROS 的水平，并恢复线粒体膜电位。NF-κB-IN-20 可用于急性肺损伤 (ALI) 的研究。

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NF-κB-IN-20

NF-κB-IN-20 Chemical Structure

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NF-κB-IN-20 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Heme Oxygenase (HO) 亚型特异性产品:

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HO-1 HO-2

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

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NF-κB-IN-20 is an orally active NF-κB inhibitor. NF-κB-IN-20 directly binds to the Keap1 protein, activating the Keap1/Nrf2/HO-1 antioxidant pathway, and simultaneously inhibiting the NF-κB inflammatory pathway, thereby synergistically reducing oxidative stress and inflammatory responses. NF-κB-IN-20 M11 inhibits the expression of IL-6, IL-1β, and TNF-α, significantly reduces the level of ROS, and restores the mitochondrial membrane potential. NF-κB-IN-20 can be used for the study of acute lung injury (ALI)[1].

IC50 & Target[1]

NF-κB

 

IL-6

 

IL-1β

 

HO-1

 

体外研究
(In Vitro)

NF-κB-IN-20 (Compound M11) (0.01‑100 μM, 5 h) 在 LPS (HY-D1056) 诱导的 Raw264.7 细胞中表现出良好的体外安全性 (半数致死浓度 CC50 > 100 μM) ，能够以剂量依赖的方式降低炎症和氧化应激标志物 IL-6 (IC50 = 6.55 μM) 、IL-1β、TNF-α 和 SOD 的 mRNA 表达水平，并抑制活性氧 (ROS) 的表达，增强线粒体膜电位，从而减轻 LPS 引起的细胞损伤[1]。

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

NF-κB-IN-20 相关抗体:

RT-PCR[1]

Cell Line: Raw264.7 cells
Concentration: 25, 50 and 100 μM
Incubation Time: 1 h and stimulated with LPS for 4 h.
Result: Reduced the mRNA expressions of IL-6, IL-1β, and TNF-α and increased the mRNA expression of SOD.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. AUC0-t 142 ng·h/mL
Mice 5 mg/kg p.o. AUC0-t 14 ng·h/mL
Mice 1 mg/kg i.v. AUC0-∞ 144 ng·h/mL
Mice 5 mg/kg p.o. AUC0-∞ 16 ng·h/mL
Mice 1 mg/kg i.v. Cmax 184 ng/mL
Mice 5 mg/kg p.o. Cmax 35 ng/mL
Mice 1 mg/kg i.v. T1/2 0.33 h
Mice 5 mg/kg p.o. T1/2 0.51 h
Mice 1 mg/kg i.v. Vd 3332.24 mL/kg
Mice 5 mg/kg p.o. Tmax 0.25 h
Mice 1 mg/kg i.v. CL 7069.13 mL/h/kg
Mice 5 mg/kg p.o. F 1.99 %
体内研究
(In Vivo)

NF-κB-IN-20 (Compound M11) (15-60 mg/kg, i.g., 每日一次共 7 天) 能够减轻由急性肺损伤引起的小鼠肺部损伤和氧化应激，并抑制胶原蛋白的形成以及 M1 型巨噬细胞的极化[1]。
NF-κB-IN-20 (15-60 mg/kg, i.g., 每日一次共 7 天) 能够增加小鼠的痰液分泌，并减轻咳嗽症状，从而有助于肺部疾病的治疗[1]。
NF-κB-IN-20 (500 mg/kg, i.g., 单次剂量) 在 SD 大鼠的 14 天观察期内显示出良好的体内安全性特征[1]。

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

Animal Model: LPS induced ALI model established in five-to six-week-old male BALB/c mice[1]
Dosage: 15, 30 and 60 mg/kg
Administration: Oral gavage (i.g.), once daily for 7 days
Result: Significantly reduced the total number of inflammatory cells in BALF.
Enhanced the activities of SOD and GSH-Px in lung tissue, while reducing the level of ROS, effectively reversing the oxidative stress caused by LPS.
Improved the pathological phenomena such as inflammatory cell infiltration, destruction of alveolar structure, and thickening of alveolar septa.
Inhibited the expression of M1-type macrophage markers (iNOS, CD86), while promoting the expression of M2-type markers (Arg-1, CD163).
Animal Model: Cecal puncture induced ALI model established in five-to six-week-old male BALB/c mice[1]
Dosage: 15, 30 and 60 mg/kg
Administration: Oral gavage (i.g.), once daily for 7 days
Result: Alleviated lung injury caused by sepsis infection.
Ameliorated inflammatory cell infiltration, alleviated alveolar atrophy, and inhibited collagen formation and fibrosis.
Reversed the expression of inflammatory cytokine and oxidative stress related factors.
Animal Model: 5 % ammonia-induced cough assay established in five-to six-week-old male BALB/c mice[1]
Dosage: 15, 30 and 60 mg/kg
Administration: Oral gavage (i.g.), once daily for 7 days
Result: Demonstrated a significant increase in phenol red secretion in the BALF.
Led to a prolonged cough latency period and a decreased frequency of coughs.
分子量

353.41

Formula

C21H23NO4
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

NF-κB-IN-20 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

NF-κB-IN-20NF-κBKeap1-Nrf2Heme Oxygenase (HO)Interleukin RelatedTNF ReceptorReactive Oxygen Species (ROS)SODNuclear factor-κBNuclear factor-kappaBHeme OxygenaseILTumor Necrosis Factor ReceptorTNFRSuperoxide DismutaseAcute lung injuryAnti-inflammationLansiummaide B analoguesOxidative stressInhibitorinhibitorinhibit

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