HIF inhibitors and activators

Use this guide to find the right compound to activate or inhibit the Hypoxia Inducible Factor (HIF) signaling pathway.

Multiple pharmacological compounds can activate or inhibit proteins involved in HIF signaling regulation. The table below highlights some of the small molecules that can be used to study the HIF pathway.​

​​HIF inhibitors

Small moleculeDescription
CAY10585Suppresses transcription of HIF-1 target genes VEGF and erythropoietin
ChetominPotent HIF inhibitor; reduces CA9 and VEGF expression in hypoxic cells
ChrysinIncreases HIF-1α degradation via increase in prolyl hydroxylation
Dimethyloxaloylglycine (DMOG)Cell-permeable prolyl hydroxylase (PHD) inhibitor
Dimethyl-bisphenol APromotes degradation of HIF-1α protein by dissociating Hsp90 from HIF-1α
EchinomycinPotent, reversible cell-permeable HIF-1α inhibitor (EC50 = 1.2 nM)
PX 12Irreversible, competitive Thioredoxin-1 inhibitor; attenuates HIF-1 expression
Vitexin (Apigenin 8-C-glucoside)Antioxidative and anti-inflammatory HIF-1α inhibitor
YC-1Reduces HIF-1α and HIF-2α expression; inhibits HIF-1α via FIH-dependent CAD inactivation

Other HIF signaling tools

Small moleculeDescription
Deferoxamine mesylate (DFO)Iron chelator also used as hypoxia-mimetic agent (HIF-1α activator)

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