328501 Sigma-AldrichERO1 Inhibitor II, EN460 - Calbiochem
Sinonimi: (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
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Panoramica
Replacement Information |
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Tabella delle specifiche principali
Empirical Formula |
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C₂₂H₁₂ClF₃N₂O₄ |
Products
Numero di catalogo | Confezionamento | Qtà/conf | |
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328501-25MG | Bottiglia di vetro | 25 mg |
Description | |
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Overview | A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1α and inhibits its activity (IC50 = 1.9 µM). 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 ERO1α even in the presence of an excess amount of competing thiols. Can inhibit ERO1α even in the presence of an excess amount of competing thiols. EN460 binding to ERO1α 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. |
Catalogue Number | 328501 |
Brand Family | Calbiochem® |
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 |
References | |
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References | Chu, Y., et al. 2011. Bioorg. Med. Chem. Lett. 21, 1118. Blais, J.D., et al. 2010. J. Biol. Chem. 285, 20993. |
Product Information | |
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Form | Red solid |
Hill Formula | C₂₂H₁₂ClF₃N₂O₄ |
Chemical formula | C₂₂H₁₂ClF₃N₂O₄ |
Structure formula Image | |
Quality Level | MQ100 |
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Biological Information | |
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Purity | ≥99% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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Numero di catalogo | GTIN |
328501-25MG | 04055977195644 |
Documentation
ERO1 Inhibitor II, EN460 - Calbiochem MSDS
Titolo |
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ERO1 Inhibitor II, EN460 - Calbiochem Certificati d'Analisi
Titolo | Numero di lotto |
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328501 |
Riferimenti bibliografici
Panoramica delle referenze |
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Chu, Y., et al. 2011. Bioorg. Med. Chem. Lett. 21, 1118. Blais, J.D., et al. 2010. J. Biol. Chem. 285, 20993. |