1-Chloro-3-methanesulfonyl-6,6-dimethyl-6,7-dihydro-5H-benzo[c]thiophen-4-one

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.

AI-3 is an electrophilic, antioxidant response element (ARE) activator. AI-3 has the potential to become a valuable biological tool regarding the development of therapeutics towards oxidative stress related diseases.

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