2. NF-κB Neuronal Signaling Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  3. Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase
  4. Keap1/Nrf2/ARE activator 2

Keap1/Nrf2/ARE activator 2 是一种 Keap1/Nrf2/ARE 通路激活剂，以非竞争性方式抑制 AChE，IC50 值为 14.79 μM，Ki 值为 1.35 μM。Keap1/Nrf2/ARE activator 2 可促进 Nrf2 核转位，从而上调抗氧化基因表达，增强细胞对氧化应激的防御能力。Keap1/Nrf2/ARE activator 2 对 PC12 细胞中由 H2O2 和 Scopolamine (SCA) (HY-N0296) 诱导的损伤均表现出显著的神经保护作用。在斑马鱼模型中，Keap1/Nrf2/ARE activator 2 可改善 SCA 诱导的认知功能障碍相关的记忆障碍和神经炎症。Keap1/Nrf2/ARE activator 2 可用于阿尔茨海默病的研究。

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Keap1/Nrf2/ARE activator 2

Keap1/Nrf2/ARE activator 2 Chemical Structure

CAS No. : 3105470-83-2

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Keap1/Nrf2/ARE activator 2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

IL-6

 

IL-1β

 

AChE

14.79 μM (IC50)

AChE

1.35 μM (Ki)

HO-1

 

NQO1

 

体外研究
(In Vitro)

Keap1/Nrf2/ARE activator 2 (compound 32) (5-100 µM，24 小时) 在浓度高达 20 μM 时对 PC12 细胞未显示出明显的毒性作用[1]。
Keap1/Nrf2/ARE activator 2 (5-20​​ µM，24 小时) 对 H2O2 和 SCA 诱导的 PC12 细胞损伤表现出显著的细胞保护作用，表现为细胞活力提高、LDH 和 ROS 释放减少和细胞凋亡抑制[1]。
Keap1/Nrf2/ARE activator 2 (20 µM，2-8 小时) 以时间依赖性方式诱导 PC12 细胞中 Nrf2 的积累和核转位[1]。
Keap1/Nrf2/ARE activator 2 (20 µM，6-24 小时) 可在 PC12 细胞中上调多种抗氧化系统，如 HO-1、NQO1、Trx、TrxR 和 GCLC mRNA[1]。

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

Keap1/Nrf2/ARE activator 2 相关抗体:

Cell Viability Assay[1]

Cell Line: PC12, PC12-siNrf2 and PC12-siNT cells
Concentration: 5, 10, 20, 50, 100 µM
Incubation Time: 24 h
Result: Displayed no significant toxic effect on PC12 cells upto 20 μM following 24 h exposure.
Rescued PC12 cells from the H2O2-induced oxidative damages.
Demonstrated robust protection against SCA-induced cytotoxicity.
Significantly protected the control cells from the H2O2-induced injury, while showing no protective effect in the Nrf2-deficient cells.
Showed a protective effect in PC12-siNrf2 cells.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 5, 10, 20 µM
Incubation Time: 2, 4, 8 h
Result: Significantly activated the Nrf2/ARE signaling pathway.
Showed a marked increase in total and nuclear Nrf2 levels as early as 2 h after treatment.

Real Time qPCR[1]

Cell Line: PC12 cells
Concentration: 20 µM
Incubation Time: 6, 12, 24 h
Result: Significantly upregulated HO-1, NQO1, Trx, TrxR, and GCLC mRNA after 6 h.
体内研究
(In Vivo)

Keap1/Nrf2/ARE activator 2 (5 μM，48 小时) 通过减少神经炎症、恢复胆碱能功能和激活 Nrf2/ARE 抗氧化通路，改善了 SCA 诱导斑马鱼模型中的认知障碍[1]。

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

Animal Model: Adult AB-strain zebrafish (6-months old) challenged with SCA (200 μM in water)[1]
Dosage: 5 μM
Administration: 48 h
Result: Significantly improved spatial memory performance in zebrafish challenged with scopolamine, as evidenced by increased preference for the target arm in the T-maze test and enhanced orientation.
Restored swimming velocities, suggesting improved motor function.
Reduced neuroinflammation by attenuating the expression of IL-1β, IL-6, TNF-α and upregulated the expression of antioxidant genes (Nrf2, Gpx4, Trx).
Restored AChE activity to near-physiological levels.
分子量

333.13

Formula

C15H9BrO4
CAS 号
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

Keap1/Nrf2/ARE activator 2 相关分类

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  • 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:

Keap1/Nrf2/ARE activator 23105470-83-2Keap1-Nrf2Cholinesterase (ChE)Interleukin RelatedTNF ReceptorReactive Oxygen Species (ROS)Heme Oxygenase (HO)Quinone ReductaseILTumor Necrosis Factor ReceptorTNFRHeme OxygenaseAChEOxidative stressNrf2NeuroprotectionInhibitorinhibitorinhibit

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