AI-3 (882288-28-0) is an activator of antioxidant response element (ARE) which induces cytoprotective genes in human cells. It alkylates Keap1 at Cys151 and is reactive toward additional cysteines at higher concentrations. Disrupts Nrf2/Keap1 and Keap1/Cul3 interactions and stabilizes Nrf2. AI-3 activates ARE in an Nrf2 and PI 3-kinase dependent manner. Cell permeable and active in vivo.
1) Wang et al. (2013), In vitro and in vivo characterization of a tunable dual-reactivity probe of the Nrf2-ARE pathway; ACS Chem. Biol., 8 1764