The Keap1–Nrf2 interaction plays important roles in regulation of Nrf2 activity and induction of chemopreventive enzymes. Keap1 is known to mediate the ubiquitination of Nrf2, a master regulator of the antioxidant response. Directly interrupting the Keap1–Nrf2 interaction has been emerged as a promising strategy to develop novel class of antioxidant, antiinflammatory, and anticancer agents.