产品说明
一般描述
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.
包装
25 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
Keap1
Reversible: no
警告
Toxicity: Standard Handling (A)
重悬
Use only fresh DMSO for reconstitution.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Hur, W., et al. 2010. Chem. Biol.17, 537.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C13H12ClNO3 |
分子量 | 265.69 |
MDL编号 | MFCD00634787 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze desiccated protect from light |
颜色 | off-white |
溶解性 | DMSO: 50 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
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 key | XUJQDJGGHFNYDY-UHFFFAOYSA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
Sigma-Aldrich