Keap1-IN-1

Keap1-IN-1 (Compound 27) is a covalent Keap1 inhibitor that selectively targets the Cys151 residue, disrupting the Keap1-Nrf2 interaction to activate the Nrf2/ARE pathway. It induces NQO1 expression (EC50 = 160 nM) and demonstrates cytotoxicity in U2OS cells (EC50 = 527 nM), making it a valuable chemical probe for studying oxidative stress responses in cancer and neurodegenerative disease research.