Chemical Name: (E)-2-(2,4-Dichlorophenyl)-4-((5-phenylfuran-2-yl)methylene-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one
ERO1A inhibitor
Molekulargewicht:
451.23
Reinheit:
98% by TLC NMR (Conforms)
Formulierung:
Orange/red solid
Formel:
C21H11Cl2F3N2O2
Anwendungsbeschreibung:
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.
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