328501

ERO1 Inhibitor II, EN460

• 別名: ERO1 Inhibitor II, EN460, ( 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, (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
• 実験式（ヒル表記法）: C₂₂H₁₂ClF₃N₂O₄
• 分子量: 460.79
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• アッセイ: ≥99% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: red
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

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.

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

Chu, Y., et al. 2011. Bioorg. Med. Chem. Lett.21, 1118.
Blais, J.D., et al. 2010. J. Biol. Chem.285, 20993.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable