This guide is intended as a navigator to finding the right compound to activate or inhibit the Hypoxia Inducible Factor (HIF) signaling pathway.
A great number of pharmacological compounds can activate or inhibit proteins involved in HIF signaling regulation. The table below presents the highlights of the small molecules that can be used to study the HIF pathway.
||Suppresses transcription of HIF-1 target genes VEGF and erythropoietin
||Potent HIF inhibitor; reduces CA9 and VEGF expression in hypoxic cells
||Increases HIF-1α degradation via increase in prolyl hydroxylation
||Cell-permeable prolyl hydroxylase (PHD) inhibitor
||Promotes degradation of HIF-1α protein by dissociating Hsp90 from HIF-1α
||Potent, reversible cell-permeable HIF-1α inhibitor (EC50 = 1.2 nM)
||Irreversible, competitive Thioredoxin-1 inhibitor; attenuates HIF-1 expression
|Vitexin (Apigenin 8-C-glucoside)
||Antioxidative and anti-inflammatory HIF-1α inhibitor
||Reduces HIF-1α and HIF-2α expression; inhibits HIF-1α via FIH-dependent CAD inactivation
Other HIF Signaling Tools
|Deferoxamine mesylate (DFO)
||Iron chelator also used as hypoxia-mimetic agent (HIF-1α activator)
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