Biochem/physiol Actions

Hypoxia inducible transcription factors (HIF) control gene expression when oxygen availability is low and are associated with the onset and progression of a variety of cancers. They are heterodimers of an HIF-A (HIF-1A, HIF-2A also known as EPAS-1, or HIF-3A) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β). N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine is a highly selective antagonist of HIF-2 heterodimerization, DNA-binding activity, and target gene transcription. It binds the HIF-2A PAS-B domain with a KD ~80 nM compared to a KD > 5000 nM for the HIF-1A PAS-B domain.

Features and Benefits

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Packaging

5, 25 mg in glass bottle