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EN460

 - ERO1 Inhibitor II
Axon 2737
CAS:  496807-64-8
Purity:  99%
  • Soluble in DMSO
  • MF:  C22H12ClF3N2O4
  • MW:  460.79

Description

EN460 is an inhibitor of endoplasmic reticulum oxidoreductin-1α (ERO1α) with an IC50 value of 1.9 µM. It preferentially interacts with the reduced, catalytically active form of ERO1α and prevents enzyme reoxidation, thereby perturbing oxidative protein folding in the endoplasmic reticulum.

EN460 is used to study ERO1α-dependent disulfide-bond formation, redox homeostasis and endoplasmic-reticulum stress. Because the compound reacts rapidly with thiolates and can display broader thiol reactivity, orthogonal target-engagement controls are important when assigning ERO1-specific cellular effects.

Key Features

  • ERO1α inhibitor (IC50: 1.9 µM)
  • Targets the reduced active enzyme state
  • Perturbs oxidative protein folding
  • Thiol-reactive chemical probe

Applications

  • ERO1α enzymology
  • Endoplasmic-reticulum redox studies
  • Oxidative protein-folding research
  • Unfolded protein response assays
  • Target-engagement and thiol-reactivity studies

More Information

Parent CAS No. 496807-64-8
Chemical Name (Z)-2-Chloro-5-(5-oxo-4-((5-phenylfuran-2-yl)methylene)-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
SMILES C1C(N2N=C(C(F)(F)F)/C(=C/C3=CC=C(C4C=CC=CC=4)O3)/C2=O)=CC=C(Cl)C=1C(O)=O
MFCD N.A.
InChi InChI=1S/C22H12ClF3N2O4/c23-17-8-6-13(10-15(17)21(30)31)28-20(29)16(19(27-28)22(24,25)26)11-14-7-9-18(32-14)12-4-2-1-3-5-12/h1-11H,(H,30,31)/b16-11-
InChiKey RSLFQCNAOMQAIH-WJDWOHSUSA-N
CID 1016023
Short Description ERO1 inhibitor

Other Categories

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Axon Ligands™ for Cell Signaling & Oncology

Axon Ligand™ for Stem Cell Research 

Axon Ligands™ for Epigenetic Research 

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