I2 | ERO1A inhibitor

CAS:
 N/A
Catalog Number:
 10-4908

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I2 is an inhibitor of the oxidoreductase ERO1A (IC50 = 8.1 µM), a mediator of the unfolded protein response (UPR).1 Under cancer-related hypoxia conditions, ERO1A favors the folding of the angiogenic protein VEGFA leading to cancer cell growth and spread. I2 inhibited the metabolic activity of DMA-MB-231 triple negative breast cancer cells and impaired migration and VEGF secretion.  Tumors in C57/BL6Jmice showed decreased levels of VEGF and PD-L1 when treated with I2.

References/Citations:

  1. Varone et al. (2025), Small molecule-mediated inhibition of the oxidoreductase ERO1A restrains aggressive breast cancer by impairing VEGF and PD-L1 in the tumor microenvironment; Cell Death Dis. 16 105
ERO1A inhibitor, I2 ERO1A inhibitor, I2 supplier, oxidoreductase inhibitor
CAS:
N/A
Catalog Number:
10-4908
Activity:
ERO1A inhibitor
Chemical Names:
(E)-2-(2,4-Dichlorophenyl)-4-((5-phenylfuran-2-yl)methylene-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one
Molecular Weight:
451.23
Molecular Formula:

C21H11Cl2F3N2O2

Solubility:
Soluble in DMSO (15 mg/ml with warming)
Physical Properties:
Orange/red solid
Purity:

98% TLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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I2 is an inhibitor of the oxidoreductase ERO1A (IC50 = 8.1 µM), a mediator of the unfolded protein response (UPR).1 Under cancer-related hypoxia conditions, ERO1A favors the folding of the angiogenic protein VEGFA leading to cancer cell growth and spread. I2 inhibited the metabolic activity of DMA-MB-231 triple negative breast cancer cells and impaired migration and VEGF secretion.  Tumors in C57/BL6Jmice showed decreased levels of VEGF and PD-L1 when treated with I2.

References/Citations:

  1. Varone et al. (2025), Small molecule-mediated inhibition of the oxidoreductase ERO1A restrains aggressive breast cancer by impairing VEGF and PD-L1 in the tumor microenvironment; Cell Death Dis. 16 105

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