Compound or Inhibit the Hypoxia Inducible Factor (HIF)

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.

HIF Inhibitors

Small molecule Description
CAY10585 Suppresses transcription of HIF-1 target genes VEGF and erythropoietin
Chetomin Potent HIF inhibitor; reduces CA9 and VEGF expression in hypoxic cells
Chrysin Increases HIF-1α degradation via increase in prolyl hydroxylation
Dimethyloxaloylglycine (DMOG) Cell-permeable prolyl hydroxylase (PHD) inhibitor
Dimethyl-bisphenol A Promotes degradation of HIF-1α protein by dissociating Hsp90 from HIF-1α
Echinomycin Potent, reversible cell-permeable HIF-1α inhibitor (EC50 = 1.2 nM)
PX 12 Irreversible, competitive Thioredoxin-1 inhibitor; attenuates HIF-1 expression
Vitexin (Apigenin 8-C-glucoside) Antioxidative and anti-inflammatory HIF-1α inhibitor
YC-1 Reduces HIF-1α and HIF-2α expression; inhibits HIF-1α via FIH-dependent CAD inactivation

Other HIF Signaling Tools

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

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Last updated: Apr 1, 2019 at 6:00 AM

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