492041

Nrf2 Activator II, AI-1

The Nrf2 Activator II, AI-1, also referenced under CAS 75483-04-4, modulates the biological activity of Nrf2. This small molecule/inhibitor is primarily used for Biochemicals applications.

• 同義詞: Nrf2 Activator II, AI-1, Ethyl-4-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate
• 經驗公式（希爾表示法）: C₁₃H₁₂ClNO₃
• CAS號碼: 75483-04-4
• 分子量：: 265.69
• MDL號碼: MFCD00634787
• 分類程式碼代碼: 12352200
• NACRES: NA.51

屬性

• 品質等級: 100
• 化驗: ≥97% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated; protect from light
• 顏色: off-white
• 溶解度: DMSO: 50 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• InChI: 1S/C13H12ClNO3/c1-3-18-13(17)10-11(14)8-6-4-5-7-9(8)15(2)12(10)16/h4-7H,3H2,1-2H3
• InChI 密鑰: XUJQDJGGHFNYDY-UHFFFAOYSA-N

描述

一般說明

A cell-permeable chloro-quinolinone compound that selectively and covalently modifies Kelch-like ECH-associated protein 1 (Keap1)-Cys¹⁵¹ and represses Keap1 function and reduces Nrf2 (Nuclear factor E2-related factor 2)-Keap1 interaction. Shown to stabilize Nrf2 by inhibiting the Keap1-driven ubiquitination of Nrf2 and thereby activating the Nrf2-ARE (antioxidant response element) pathway (EC₅₀ = 2.7 µM in neuroblastoma IMR-32 cells). Offers protection against H₂O₂ induced oxidative stress, but unlike tert-butylhydroquinone (Cat. No. 286888) AI-1 does not act as a free radical scavenger. Its anti-oxidant effects are mediated via Nrf2 induced antioxidant response. Does not affect mutant ARE where GC are substituted with AT within the core ARE sequence.

A cell-permeable chloro-quinolinone compound that selectively and covalently modifies Kelch-like ECH-associated protein 1 (Keap1)-Cys¹⁵¹ and represses Keap1 function and reduces Nrf2 (Nuclear factor erythroid 2-related factor 2)-Keap1 interaction. Shown to stabilize Nrf2 by inhibiting the Keap1-driven ubiquitination of Nrf2 and thereby activating the Nrf2-ARE (antioxidant response element) pathway (EC₅₀ = 2.7 µM in neuroblastoma IMR-32 cells). Offers protection against H₂O₂ induced oxidative stress, but unlike tert-butylhydroquinone (Cat. No. 286888). AI-1 does not act as a free radical scavenger. Its anti-oxidant effects are mediated via Nrf2 induced antioxidant response. Does not affect mutant ARE where GC are substituted with AT within the core ARE sequence.

生化／生理作用

Cell permeable: yes

Primary Target
Keap1

Reversible: no

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

其他說明

Hur, W., et al. 2010. Chem. Biol.17, 537.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3