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EN460 EN460 is a small molecule inhibitor by EN460 binding to ERO1α to promote the loss of flavin adenine dinucleotide (FAD) from the holoenzyme(IC50=1.9 uM). Uses: Ero1 inhibitor ii. Synonyms: EN460; EN-460; EN 460. 2-chloro-5-[5-oxo-4-[(5-phenyl-2-furyl)methylene]-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid. Grades: ≥98%. CAS No. 496807-64-8. Molecular formula: C22H12ClF3N2O4. Mole weight: 460.79. BOC Sciences 9
ERO1 Inhibitor II, EN460 A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1alpha and inhibits its activity (IC50 = 1.9uM). Also prevents ERO1 re-oxidation both in vitro and in mouse embryonic fibroblasts. Activates the unfolded protein response and protects ER-stressed 293T cells. Can inhibit ERO1alpha even in the presence of an excess amount of competing thiols. Can inhibit ERO1alpha even in the presence of an excess amount of competing thiols. EN460 binding to ERO1alpha is shown to promote the loss of flavin adenine dinucleotide (FAD) from the holoenzyme. Its inhibitory action appears to be irreversible, however addition of FAD and tris (hydroxypropyl) phosphine can restore some enzyme activity. Group: Biochemicals. Alternative Names: (Z)-2-Chloro-5-(4,5-dihydro-5-oxo-4-((5-phenyl-2-furanyl)methylene)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzoic Acid, (Z)-2-Chloro-5-(5-oxo-4-((5-phenylfuran-2-yl)methylene)-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl)benzoic Acid. Grades: Highly Purified. CAS No. 496807-64-8. Pack Sizes: 25mg. Molecular Formula: C??H??ClF?N?O?, Molecular Weight: 460.8. US Biological Life Sciences. USBiological 4
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