Nrf2 Activator II, AI-1 (Ethyl-4-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate)
Description
Purity ~97% (HPLC). 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 = 2.7uM in neuroblastoma IMR-32 cells). Offers protection against H2O2 induced oxidative stress, but unlike tert-butylhydroquinone 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. Formula: C13H12ClNO3 Molecular Weight: 265.7 Solubility: DMSO (50mg/ml)