Chemical Name: N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
Biological ActivityHigh affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Allosteric inhibition of hypoxia inducible factor-2 with small molecules.
Scheuermann TH, Li Q, Ma HW et al.
Nat Chem Biol
Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor.
Rogers et al.
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