1422955-31-4

HIF-2α-I2 (1422955-31-4) is a potent and selective HIF-2α inhibitor, Kd=81 nM.1?Binds to the HIF-2α PAS-B domain2?and interferes with Hif-2α / ARNT heterodimerization reducing target gene expression in a cellular model1. Highly selective for HIF-2α displaying a >60-fold selectivity over HIF-1α.1,2

N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine is a HIF-2α inhibitor which inhibits HIF-2α-ARNT heterodimerization by binding to HIF-2α PAS-B domain. It may be used in therapeutic treatment of HIF-2-driven tumors such as renal cell carcinomas.

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1) Scheuermann?et al.?(2013),?Allosteric inhibition of hypoxia inducible factor-2 with small molecules; Nat. Chem. Biol.,?9?271 2) Masetti?et al.?(2014),?Protein dynamics of the HIF-2α PAS-B domain upon heterodimerization and ligand binding; PLoS One,?9(4)?e94986 3) Rodgers?et al.?(2013),?Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor; J. Med. Chem.,?56 1739