1. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. NF-κB Heme Oxygenase (HO) Interleukin Related Reactive Oxygen Species (ROS) NO Synthase
  3. Nrf2 activator-24

Nrf2 activator-24 是一种具有抗炎抗氧化活性的 Nrf2 激活剂。Nrf2 activator-24 可促进 Nrf2 的核转位,进而诱导下游抗氧化和细胞保护基因的表达。Nrf2 activator-24 可抑制角质形成细胞中细胞因子驱动的炎症反应。Nrf2 activator-24 可减轻巨噬细胞中的炎症、亚硝化和氧化应激反应。Nrf2 activator-24 可缓解 DNCB 诱导的小鼠模型中的局部炎症及特应性皮炎样症状。Nrf2 activator-24 可用于特应性皮炎的相关研究。

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Nrf2 activator-24

Nrf2 activator-24 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nrf2 activator-24 is a Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-24 promotes the nuclear translocation of Nrf2, thereby inducing the expression of downstream antioxidant and cytoprotective genes. Nrf2 activator-24 inhibits cytokine-driven inflammatory responses in keratinocytes. Nrf2 activator-24 attenuates inflammation, nitrosation and oxidative stress responses in macrophages. Nrf2 activator-24 alleviates local inflammation and atopic dermatitis-like symptoms in DNCB-induced mouse models. Nrf2 activator-24 can be used in research related to atopic dermatitis[1].

体外研究
(In Vitro)

Nrf2 activator-24 (compound 5w) (6 h) 可在基因工程化 U2OS 细胞中强效诱导 Nrf2 核转位,其 EC50 为 4.9 nM[1]
Nrf2 activator-24 (0-1 μM; 24 h) 对人角质形成细胞 HaCaT 无细胞毒性[1]
Nrf2 activator-24 (0.003-0.1 μM; 0-24 h) 可在处理后 3 h 诱导人角质形成细胞 HaCaT 中 Nrf2 核转位达到峰值,此后直至 24 h 其水平逐渐下降[1]
Nrf2 activator-24 (0.03-1 μM;6-12 h) 可在人角质形成细胞 HaCaT 中诱导 Nrf2、HO-1 和 GCLM 蛋白表达呈浓度依赖性升高,在 1 μM 时效应达到最大值[1]
Nrf2 activator-24 (0.03-1 μM;6 h) 可在人角质形成细胞 HaCaT 中诱导 HMOX1、GCLM、GCLC 和 NQO1 的 mRNA 表达呈浓度依赖性升高,在 1 μM 时作用达到峰值[1]
Nrf2 activator-24 (0.03-1 μM; 3 h) 可浓度依赖性地抑制经 TNF-α+IFN-γ 刺激的人角质形成细胞 HaCaT 中 IL-1β 的蛋白表达,IL-6 的分泌[1]
Nrf2 activator-24 (0.03-1 μM; 6 h) 可浓度依赖性地抑制经 TNF-α+IFN-γ 刺激的人角质形成细胞 HaCaT 中 IL6、TNF、CCL17 和 CCL22mRNA 表达[1]
Nrf2 activator-24 (0.03-1 μM; 3 h) 可浓度依赖性地抑制 LPS (HY-D1056) 刺激的 Raw264.7 小鼠巨噬细胞中 iNOS 蛋白的表达[1]
Nrf2 activator-24 (0.03-1 μM; 3 h) 可浓度依赖性地抑制 LPS 刺激的 Raw264.7 小鼠巨噬细胞中 NO 的生成[1]
Nrf2 activator-24 (0.1 μM; 9 h) 可有效降低 Raw264.7 小鼠巨噬细胞中由 H2O2 诱导的细胞内 ROS 水平[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: HaCaT human keratinocytes
Concentration: up to 1 μM
Incubation Time: 24 h
Result: Showed no cytotoxic effects on HaCaT keratinocytes at concentrations up to 1 μM.

Western Blot Analysis[1]

Cell Line: HaCaT human keratinocytes
Concentration: 0.003, 0.01, 0.03, 0.1 μM
Incubation Time: 3 h
Result: Increased nuclear Nrf2 in a concentration-dependent manner.
Induced a significant 3.60 ± 0.11-fold increase in nuclear Nrf2 at 0.003 μM.

Western Blot Analysis[1]

Cell Line: HaCaT human keratinocytes
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 6 h (Nrf2); 12 h (HO-1, GCLM)
Result: Increased Nrf2 protein accumulation to 5.71 ± 0.10-fold at 1 μM (6 h treatment).
Upregulated HO-1 and GCLM expression by 10.58 ± 0.74-fold and 3.44 ± 0.11-fold, respectively, at 1 μM (12 h treatment).

Western Blot Analysis[1]

Cell Line: TNF-α+IFN-γ-stimulated HaCaT human keratinocytes
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 3 h pretreatment; 24 h cytokine stimulation
Result: Suppressed TNF-α+IFN-γ-induced IL-1β protein expression in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: LPS-stimulated Raw264.7 mouse macrophages
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 3 h pretreatment; 24 h LPS stimulation
Result: Suppressed LPS-induced iNOS protein expression in a concentration-dependent manner.
体内研究
(In Vivo)

Nrf2 activator-24 (0.1-0.5%;局部给药;每 2 天 1 次;第 8-14 天) 可有效缓解 DNCB 诱导的 BALB/c 小鼠特应性皮炎样症状[1]

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

Animal Model: BALB/c (6-week-old male, DNCB-induced atopic dermatitis model)[1]
Dosage: 0.1%; 0.5%
Administration: topical; every other day; Days 8-14, 1 hour after DNCB challenge
Result: Significantly reduced dermatitis scores.
Significantly suppressed scratching behavior.
Reduced spleen and lymph node weights in a concentration-dependent manner.
Significantly lowered plasma IgE levels.
Significantly attenuated epidermal thickening.
Significantly reduced eosinophil infiltration in dorsal skin.
Significantly reduced mast cell infiltration in dorsal skin (0.5% group); showed near-significant reduction (0.1% group).
Significantly reduced skin IL-6 protein levels in a concentration-dependent manner.
Significantly restored skin loricrin protein levels.
分子量

360.09

Formula

C14H10Cl2O2Se

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
  • 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.

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产品名称:
Nrf2 activator-24
目录号:
HY-182040
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