RTA 408 is a synthetic triterpenoid that binds Keap1 and attenuates the degradation of Nrf2 at concentrations ≤25 nM. In this way, it suppresses the generation of nitric oxide and pro-inflammatory cytokines in macrophages stimulated with IFN-γ. At higher concentrations, RTA 408 inhibits tumor cell growth (GI50 = 260 nM), blocks NF-κB signaling, and decreases levels of cyclin D1. Topical application of RTA 408 activates Nrf2 and provides cytoprotective effects.
