The KEAP1-Nrf2 pathway is the major regulator of cytoprotective responses to chemical and/or oxidative stresses caused by reactive oxygen species (ROS) and electrophiles. Nrf2 (nuclear factor erythroid 2-related factor 2) is a transcription factor that binds together with small Maf proteins to the antioxidant response element (ARE) in the regulatory regions of cellular defense enzyme genes leading to the activation of a wide rang of cell defense processes; while KEAP1 (Kelch ECH associating protein 1), a negative repressor of Nrf2, is an adaptor protein for a Cul3-based ubiqutitin E3 ligase that binds to Nrf2 and promotes its degradation by the ubiquitin proteasome pathway.
- C5715 NK 252Summary: Nrf2 activator
- C4733 SulforaphaneSummary: inducer of chemopreventative enzymes via Keap1-Nrf2 signaling
- C4354 CDDO-TFEASummary: Nrf2 activator
- C3234 2-HBASummary: indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway.
- B3576 Omaveloxolone (RTA-408)Target: Nrf2Summary: Nrf2 activator
- B1931 Dimethyl FumarateSummary: nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator
- A3335 Curcumin1 CitationTarget: Histone Deacetylases (HDACs)|Nrf2|Histone Acetyltransferases (HATs)|TyrosinasesSummary: Tyrosinase inhibitor
- A3220 BardoxoloneTarget: COX|iNOSSummary: Once-a-day treatment for CKD
- N2172 5,7-dihydroxychromone1 CitationTarget: Nrf2/ARE signal|PPARSummary: Nrf2/ARE signal activator and PPARγ agonist
- N2285 Dimethylfraxetin