An ERO1α inhibitor
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EN460

Item No. 43950

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-chloro-5-[4,5-dihydro-5-oxo-4-[(5-phenyl-2-furanyl)methylene]-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzoic acid
CAS Number
496807-64-8
Molecular Formula
C22H12ClF3N2O4
Formula Weight
460.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N(C1=CC(C(O)=O)=C(Cl)C=C1)N=C2C(F)(F)F)C2=CC3=CC=C(C4=CC=CC=C4)O3
InChi Code
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)
InChi Key
RSLFQCNAOMQAIH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $165

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    25 mg

    $310

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    Product Description

    EN460 is an inhibitor of ERO1-like protein α (ERO1α; IC50 = 1.94 µM).1 It also inhibits additional FAD-containing enzymes, including monoamine oxidase A (MAO-A), MAO-B, and lysine-specific demethylase 1 (LSD1; IC50s = 7.91, 30.59, and 4.16 µM, respectively).2 EN460 (25 µM) induces endoplasmic reticulum (ER) stress and apoptosis in U266 multiple myeloma cells. It inhibits hypoxia-induced apoptosis in HT22 cells when used at a concentration of 10 µM.3 In vivo, EN460 increases survival and decreases the number of intrahepatic metastases in a Panc02 murine pancreatic ductal adenocarcinoma (PDAC) model.4 It inhibits isoproterenol-induced ventricular fibrillation in a rat model of cardiac hypertrophy induced by thoracic aortic banding.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Blais, J.D., Chin, K.T., Zito, E., et al. A small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1) with selectively reversible thiol reactivity. The Journal of Biological Chemisty 285(27), 20993-21003 (2010).

    2. Hayes, K.E., Batsomboon, P., Chen, W.C., et al. Inhibition of the FAD containing ER oxidoreductin 1 (Ero1) protein by EN-460 as a strategy for treatment of multiple myeloma. Bioorg. Med. Chem. 27(8), 1479-1488 (2019).

    3. Zhang, N., Shentu, Y., Zhu, M., et al. Role of Ero1α in cognitive impairment induced by chronic hypoxia. Brain Res. 1797:148117, (2022).

    4. Yang, J., Xu, Y., Huo, Y., et al. ERO1L promotes hepatic metastasis through activating epithelial-mesenchymal transition (EMT) in pancreatic cancer. J. Immunol. Res. 5553425 (2021).

    5. Hamilton, S., Terentyeva, R., Bogdanov, V., et al. Ero1α-dependent ERp44 dissociation From RyR2 contributes to cardiac arrhythmia. Circ. Res. 130(5), 711-724 (2022).