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. Synonyms: (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 Molecular Formula: C22H12ClF3N2O4 Molecular Weight: 460.8 Appearance: Supplied as a red solid. Purity: 99% (HPLC) Solubility: DMSO Storage and Stability: Store at 4C under inert atmosphere. Following reconstitution, aliquot and freeze at -20C. Stock solutions are stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molecular Weight:
460.8
Purity:
99% (HPLC)
Form:
Supplied as a red solid.
CAS Number:
[496807-64-8]
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