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HIF-2α antagonist 2 is an inhibitor of hypoxia-inducible factor-2α (HIF-2α) PAS-B domain heterodimerization.1 It binds to the HIF-2α PAS-B domain (Kd = 81 nM) to inhibit heterodimerization with the aryl hydrocarbon receptor nuclear translocator (ARNT) PAS-B domain in cell-free assays when used at concentrations ranging from 0.1 to 100 µM. HIF-2α antagonist 2 (0.1-30 µM) decreases expression of the HIF-2α target gene VEGFA in 786-O renal carcinoma cells.
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1. Allosteric inhibition of hypoxia inducible factor-