RA839 is a noncovalent small molecule binder to Keap1 (Kd=6 uM) and selective activator of Nrf2 signaling.
RA839 binds noncovalently to the Nrf2-interacting kelch domain of Keap1, significantly regulates 105 probe sets in bone marrow-derived macrophages at 10 uM.
RA839 prevents the induction of both iNOS expression and nitric oxide release in response to lipopolysaccharides in macrophages.
RA839 acutely induces Nrf2 target gene expression in liver in mice.
