Cat. No. 5243
Chemical Name: N-(3-Chloro-5-fluorophenyl)-4-nitro
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739. PMID: 23363003.
Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271. PMID: 23434853.
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Keywords: TC-S 7009, supplier, TC-S7009, high, affinity, inhibits, inhibitors, HIF2α, HIF2a, HIF2alpha, PASB, hypoxia-inducible, factors, Tocris Bioscience, Hypoxia Inducible Factor Inhibitor products
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