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Nrf2 degrader

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162307

    PROTACs Keap1-Nrf2 Cancer
    Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively .
    Nrf2 degrader 1
  • HY-149508

    Keap1-Nrf2 Reactive Oxygen Species 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
  • HY-144634
    DDO-7263
    1 Publications Verification

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD) .
    DDO-7263
  • HY-111126
    K67
    1 Publications Verification

    p62 Keap1-Nrf2 Cancer
    K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
    K67
  • HY-149127

    ASC-JM17; ALZ-003

    Keap1-Nrf2 Androgen Receptor HSP Mitophagy Metabolic Disease
    Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
    Rosolutamide
  • HY-159641

    BAY-3605349

    Keap1-Nrf2 Cancer
    VVD-130037 (BAY-3605349) is an orally active covalent activator of KEAP 1 (Kelch-like ECH-associated protein 1) with anti-tumor activity. VVD-130037 degrades NRF2 (nuclear factor-erythroid 2 p45-related factor 2), resulting in significant inhibition of tumor growth in advanced solid tumors .
    VVD-130037
  • HY-141439

    Keap1-Nrf2 Inflammation/Immunology Cancer
    TBE 31 is a potent and orally active NQO1 inducer with an Dm value of 1.1 nM. TBE 31 also is a potent Nrf2 activator. TBE 31 reacts with cysteines of Keap1, impairing its ability to target nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) for degradation. TBE 31 shows cytoprotective effects .
    TBE 31

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