2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation PI3K/Akt/mTOR MAPK/ERK Pathway
  3. Aldose Reductase Reactive Oxygen Species (ROS) PI3K Akt SOD p38 MAPK Keap1-Nrf2
  4. ALR2-IN-9

ALR2-IN-9 是一种有效的 ALR2 抑制剂 (IC50 = 21.8 nM)，具有优异的抗氧化活性 (DPPH 自由基清除的 EC50 值为 2.8 μM)。ALR2-IN-9 直接与活性氧 (ROS) / 活性氮 (RNS) 相互作用，阻断自由基链式反应，并可作为内源性酶抗氧化调节剂调节过氧化氢酶 (CAT) 和超氧化物歧化酶 (SOD) 的酶功能。ALR2-IN-9 通过调节 PI3K/Akt/Nrf2 通路，在体外实验中抑制高血糖介导的线粒体超氧化物过量生成，并在体内模型中改善 CuSO4 和 H2O2 诱导的氧化应激。ALR2-IN-9 可通过调控 PMK-1 等应激反应基因延长秀丽隐杆线虫的寿命。ALR2-IN-9 是一种很有前景的抗衰老候选药物。ALR2-IN-9 可用于糖尿病并发症研究。

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ALR2-IN-9

ALR2-IN-9 Chemical Structure

CAS No. : 2135481-84-2

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ALR2-IN-9 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALR2-IN-9 is a potent ALR2 inhibitor (IC50 = 21.8 nM) with excellent antioxidant activity (EC50 for DPPH radical scavenging = 2.8 μM). ALR2-IN-9 interacts directly with Reactive Oxygen Species (ROS)/Reactive Nitrogen Species (RNS) and interrupts the free radical chain reactions, and as an endogenous enzymatic antioxidant regulator, which regulates enzyme functions of CAT and SOD. ALR2-IN-9 regulates PI3K/Akt/Nrf2 pathway to attenuate hyperglycemia-mediated mitochondrial superoxide overproduction in vitro, and ameliorates CuSO4- and H2O2-induced oxidative stress in vivo. ALR2-IN-9 prolongs lifespan of C. elegans via the regulation of stress response genes such as PMK-1. ALR2-IN-9 is a promising anti-aging drug candidate. ALR2-IN-9 can be used for diabetic complication research[1].

体外研究
(In Vitro)

ALR2-IN-9 (compound 5N-D) (2.5-10 μM，24 小时) 可改善高血糖引起的人晶状体上皮细胞 (HLECs) 的功能损伤并降低其 ROS 水平[1]。
ALR2-IN-9 (10 μM，24 小时) 通过激活 PI3K/Akt 通路来保护 HLECs 免受高糖诱导的损伤，并逆转高血糖导致的 Nrf2、HO-1 和 NQO-1 基因水平降低[1]。
ALR2-IN-9 (10 μM，1 小时) 通过显著减弱 CuSO4 诱导的斑马鱼幼体内 ROS 水平的升高，显示出强大的抗氧化功效[1]。
ALR2-IN-9 (0.2% 和 0.4% wt%，8 天) 可延长氧化应激条件下秀丽隐杆线虫的平均寿命，提高 SOD 和 CAT 活性，并降低 MDA 水平[1]。
ALR2-IN-9 (0.4% wt%，8 天) 可降低线虫体内的 ROS 水平，逆转 H2O2 介导的 AKT-1、SIR-2.1、DAF-16 和 AGE-1 基因表达的抑制，并进一步增强 H2O2 诱导的 SKN-1 和 PMK-1 基因的上调表达[1]。

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

ALR2-IN-9 相关抗体:

Cell Viability Assay[1]

Cell Line: HLECs
Concentration: 2.5, 5.0, and 10 μM
Incubation Time: 24 h
Result: Reversed this hyperglycemia-induced impairments, restoring cell viability to 85.2 % at the dose of 10 μM.

Western Blot Analysis[1]

Cell Line: HLECs
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly increased the P-PI3K/PI3K and P-Akt/Akt ratios, compared to the high glucose group.
Failed to activate both PI3K and Akt in the presence of the specific PI3K inhibitor LY294002 (HY-10108).
分子量

480.51

Formula

C25H28N4O6
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

ALR2-IN-9 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

ALR2-IN-92135481-84-2Aldose ReductaseReactive Oxygen Species (ROS)PI3KAktSODp38 MAPKKeap1-Nrf2Phosphoinositide 3-kinasePKBProtein kinase BSuperoxide DismutaseALR2antioxidantROSRNSfree radical chain reactionsPI3K/Akt/Nrf2 pathwaylifespanstress response genesHLECsC. elegansPMK-1CAToxidative stressInhibitorinhibitorinhibit

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