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EN460 is an inhibitor of ERO1-like protein alpha (ERO1alpha, IC50 = 1. µM). It also inhibits additional FAD-containing enzymes, including monoamine oxidase A (MAO-A), MAO-B, and lysine-specific demethylase 1 (LSD1, IC50s = 7. 30. and 4. µM, respectively). EN460 (25 µM) induces endoplasmic reticulum (ER) stress and apoptosis in U266 multiple myeloma cells. It inhibits hypoxia-induced apoptosis in HT22 cells when used at a concentration of 10 µM. In vivo, EN460 increases survival and decreases the number of intrahepatic metastases in a Panc02 murine pancreatic ductal adenocarcinoma (PDAC) model. It inhibits isoproterenol-induced ventricular fibrillation in a rat model of cardiac hypertrophy induced by thoracic aortic banding. InChI: InChI=1S/C22H12ClF3N2O4/c23-17-8-6-13(10-15(17)21(30)31)28-20(29)16(19(27-28)22(24,25)26)11-14-7-9-18(32-14)12-4-2-1-3-5-12/h1-11H,(H,30,31) InChIKey: RSLFQCNAOMQAIH-UHFFFAOYSA-N SMILES: O=C(N(C1=CC(C(O)=O)=C(Cl)C=C1)N=C2C(F)(F)F)C2=CC3=CC=C(C4=CC=CC=C4)O3
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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