328501
ERO1 Inhibitor II, EN460
别名:
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
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关于此项目
经验公式（希尔记法）:
C22H12ClF3N2O4
分子量:
460.79
NACRES:
NA.28
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥99% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
red
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
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.
Packaging
Packaged under inert gas
Other Notes
Chu, Y., et al. 2011. Bioorg. Med. Chem. Lett.21, 1118.
Blais, J.D., et al. 2010. J. Biol. Chem.285, 20993.
Blais, J.D., et al. 2010. J. Biol. Chem.285, 20993.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable