BAY-876
GLUT1 inhibitor / Potent inhibitor (IC50 = 2 nM) of the facilitative glucose transporter GLUT1, an enzyme frequently overexpressed in many cancers.1 It shows greater than 100-fold selectivity over GLUT2-4. BAY-876 displayed potent antitumor activity in ovarian cancer xenograft models2 and in triple negative breast cancer cells displaying high glycolytic and low oxidative phosphorylation rates3. It reduced CD4+ T cell proliferation and IFN-γ secretion via GLUT1 inhibition suggesting utility against auto-inflammatory diseases.4 BAY-876 induces disulfidptosis in SLCA11high cancer cells.5
Biochemicals & reagents
1799753-84-6
4-N-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide
1) Siebeneicher et al. (2016), Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876; ChemMedChem., 11 2261 2) Ma et al. (2018), Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876; Cancers (Basel), 11 33 3) Wu et al. (2020) GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer; Nat. Commun. 11 4205 4) Chen et al. (2023), Characterization of the effect of the GLUT-1 inhibitor BAY-876 on T cells and macrophages; Eur. J. Pharmacol., 945 175552 5) Liu et al. (2023), Actin cytoskeleton vulnerability to disulfide stress mediates disulfidptosis; Nat. Chem. Biol., 25 404
-20°C
TARGET: Glucose transporter -- PATHWAY: Disulfidptosis; Cytokine; Glucose metabolism -- RESEARCH AREA: Immunology; Cell death -- DISEASE AREA: Cancer; Inflammation