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
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.