AI-1 (Synonyms: 4-Chloro-1,2-dihydro-1-methyl-2-oxo-3-quinolinecarboxylic acid ethyl ester) |
| カタログ番号GB40096 |
AI-1（75483-04-4）は、新しい抗酸化応答要素（ARE）活性化剤であり、Keap1（Kelch-like ECH-associated protein 1）の共有結合修飾によってNrf2を活性化します。Keap1はNrf2の負の調節因子ですが、AI-1によるKeap1のCys151の修飾により、Keap1がCul3-Keap1ユビキチンリガーゼ複合体のアダプターとして機能する能力が破壊され、Nrf2の転写活性化が安定化および誘導されます。 AI-1は細胞浸透性であり、細胞生理学におけるNrf2の関与を探索するための有用な薬理学的ツールです。
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Cas No.: 75483-04-4
Sample solution is provided at 25 µL, 10mM.
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AI-1 (75483-04-4) is a novel antioxidant response element (ARE) activator which activates Nrf2 by covalently modifying Keap1 (Kelch-like ECH-associated protein 1) a negative regulator of Nrf2. Modification of Cys151 of Keap1 by AI-1 disrupts the ability of Keap1 to serve as an adaptor for Cul3-Keap1 ubiquitin ligase complex, thereby stabilizing and inducing transcriptional activation of Nrf2. AI-1 is a useful pharmacological tool for probing the involvement of Nrf2 in cellular physiology. Cell permeable.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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