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Beschreibung

A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1&alpha, and inhibits its activity (IC50 = 1.9 microM). 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 ERO1&alpha, even in the presence of an excess amount of competing thiols. Can inhibit ERO1&alpha, even in the presence of an excess amount of competing thiols. EN460 binding to ERO1&alpha, 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 (Cat. No. 598250) can restore some enzyme activity., A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1&alpha, and inhibits its activity (IC50 = 1.9 microM). 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 ERO1&alpha, even in the presence of an excess amount of competing thiols. Can inhibit ERO1&alpha, even in the presence of an excess amount of competing thiols. EN460 binding to ERO1&alpha, 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 (Cat. No. 598250) can restore some enzyme activity.