EN460_DataSheet_MedChemExpress

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Inhibitors, Agonists, Screening Libraries
Data Sheet
BIOLOGICAL ACTIVITY:
EN460 is a small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1); interacts selectively(IC50=1.9 uM) with the reduced,active form of ERO1α and prevents its reoxidation.
IC50 value: 1.9 uM [1]
Target: ERO1 inhibitor
in vitro: Exposure of cells to EN460 or QM295 resulted in the accumulation of an ERO1α form with lower mobility, indicative of the reduced state. EN460 and QM295 were also found to activate an unfolded protein response reporter in cultured 293T cells.PROTOCOL (Extracted from published papers and Only for reference)
Cell assay [1] 293T cells stably transfected with the ATF6–UPRE–luciferase reporter (a gift of Michael Bassett and Jonathan Weissman,University of California, San Francisco) were treated overnight in low serum–containing media (5%) with the indicated concentration of tunicamycin (Calbiochem) or inhibitors. Cells were lysed in 25 ml of lysis buffer (25 mm glycylglycine, 15 mm MgSO4, 4 mm EGTA, 1mm DTT, 1% Triton X–100), and luciferase was developed by addition of 25 ml of luciferase assay reagent (25 mm Gly–Gly, 15 mm MgSO4, 4 mm EGTA, 2 mm DTT, 11.7 mm potassium phosphate, 1.6 mm ATP, 0.2 mg/ml CoA, 500 μm luciferin), and luminescence was read in a 96–well white plate (Costar catalog no. 3912) on a TECAN F500 plate reader.
References:
[1]. Blais JD, et al. A small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1) with selectively reversible thiol reactivity. J Biol Chem. 2010 Jul 2;285(27):20993–1003.
Product Name:
EN460Cat. No.:
HY-12837CAS No.:
496807-64-8Molecular Formula:
C 22H 12ClF 3N 2O 4Molecular Weight:
460.79Target:
Others Pathway:
Others Solubility:
10 mM in DMSO
Caution: Product has not been fully validated for medical applications. For research use only.
Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。