Synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 (nuclear factor erythroid 2-related factor 2) and inhibits the proinflammatory transcription factor NF-κB at low concentrations. RTA 408 dose-dependently reduced NO concentrations (IC50 value 4.4 Nm). At higher concentrations, RTA 408 inhibited tumor cell growth (GI50 value 260 nM) and increased caspase activity in tumor cell lines, but not in normal primary human cells. RTA 408 is a highly effective mitigator of steady state hematopoiesis and shows normalization of the frequency of hematopoietic stem and progenitor cells in mice after administration of lethal, myeloablative doses of whole-body irradiation.

KEYWORDS: Omaveloxolone | Supplier | NRF2 acitivator | RTA 408 | RTA408 | RTA-408 | CAS [1474034-05-3] | DNA-RNA | NRF | Activator | Transcription Factors | NF-E2L2 | ROS | NO | nuclear factor erythroid 2-related factor 2 | JNK | NF-κB | inflammatory | radiation | mitigator | hematopoiesis