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KEAP1 mutation

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159641

    BAY-3605349

    Molecular Glues Keap1-Nrf2 Metabolic Disease Inflammation/Immunology Cancer
    VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
    VVD-130037
  • HY-149508

    Keap1-Nrf2 Reactive Oxygen Species (ROS) Cancer
    Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
    Nrf2-IN-3

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