VVD-130037 is a covalent molecular glue and allosteric degrader of NRF2, targeting the KEAP1 protein. By binding to KEAP1, it enhances the formation of the KEAP1-CUL3 E3 ligase complex, leading to increased ubiquitination and subsequent degradation of NRF2. This compound demonstrates KEAP1 target-binding activity in both in vitro assays and mouse models, making it a useful tool in research involving NRF2-dependent cancers, solid tumors with KEAP1 mutations, and advanced solid tumors.
VVD-130037 is a covalent molecular glue and allosteric degrader of NRF2, targeting the KEAP1 protein. By binding to KEAP1, it enhances the formation of the KEAP1-CUL3 E3 ligase complex, leading to increased ubiquitination and subsequent degradation of NRF2. This compound demonstrates KEAP1 target-binding activity in both in vitro assays and mouse models, making it a useful tool in research involving NRF2-dependent cancers, solid tumors with KEAP1 mutations, and advanced solid tumors.
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