KEAP1 Activator VVD-130037

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable and covalent activator of Kelch-like ECH associated protein 1 (KEAP1), with potential antineoplastic activity. Upon oral administration, KEAP1 activator VVD-130037 allosterically binds to KEAP1, specifically at C151, and activates KEAP1. This enhances the formation of the active KEAP1-CUL3 E3 ubiquitin ligase complex and results in the degradation of the cytoprotective transcription factor nuclear factor erythroid 2 p45-related factor 2 (NRF2), thereby inhibiting NFR2-driven tumor cell proliferation. NFR2, a pro-survival protein, is hyperactivated in various cancers and plays a key role in maintaining oxidative homeostasis and cellular metabolism.

**Synonyms:** - BAY 3605349 - BAY-3605349 - BAY3605349 - KEAP1-targeting Allosteric Molecular Glue VVD-130037 - Kelch-like ECH Associated Protein 1 Activator VVD-130037 - VVD 130037 - VVD-130037 - VVD130037