Hypoxia inducible factors (HIFs) are heterodimeric proteins belonging to the basic helix-loop-helix-PAS (bHLH/PAS) family of transcription factors that mediate the primary transcriptional response to stress caused by hypoxia (accessible O2 level < 2%). HIFs are characterized by containing two subunits, including O2-labile α subunit (HIFα) and constitutively expressed β subnit (HIFβ). Mammalian HIFα consists of three isoforms, including HIF1α, HIF2α and HIF3α, which play an essential role in the regulation of HIF activity by O2 availability. Under normal O2 tension, HIFα is hydroxylated at the two conserved proline residues within the O2-dependent degradation (ODD) domain by prolylhydroxylase domain proteins (PHDs) and undergoes proteosomal degradation catalyzed by a complex formed by E3 ubiquitin ligase and the von Hippel-Lindau protein (pVHL); while, under hypoxia, HIFα stabilizes with PHDs being deactivated and hence induce transcription of genes with adaptive functions.
- 2,4-DPDCatalog No. :C4887cell permeable, competitive inhibitor of HIF-PH
- JNJ-42041935Catalog No. :C4752Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor
- AdaptaquinCatalog No. :C4377HIF-prolyl hydroxylase-2 (PHD2) inhibitor
- Octyl-α-ketoglutarateCatalog No. :C4321prolyl hydroxylases (PHD) activator
- Daprodustat(GSK1278863)Catalog No. :B6106HIF-prolyl hydroxylase inhibitor
- FG2216Catalog No. :B5851HIF-prolyl hydroxylase inhibitorFG-2216 is a potent HIF-prolyl hydroxylase inhibitor. IC50 = 3.9 μM for PDH2 enzyme.
- BAY 87-2243Catalog No. :B1115HIF-1 inhibitor,potent and selectiveBAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation .
- DMOGCatalog No. :A4506Competitive HIF-PH inhibitor, cell-permeableProlyl 4-hydroxylase (P4H) inhibitor; inhibits hypoxia-inducible factor α (HIF-α) prolyl hydroxylase (HIF-PH).
- PX 12Catalog No. :A4509Trx-1 inhibitorCompetitive, irreversible thioredoxin-1 (Trx-1) inhibitor (Ki = 31 μM) that attenuates expression of HIF-1α, VEGF and iNOS (IC50 values are 7.2, ~10 and 18.1 μM respectively). Exhibits antitumor activity; directly inhibits tubulin polymerization in vitro and decreases tumor microvessel density in vivo.
- KC7F2Catalog No. :A4507HIF-1α inhibitorInhibitor of HIF-1α. Thought to act via down-regulation of HIF-1α protein synthesis; reduces phosphorylation of eIF4E binding protein 1 (4EBP1) and p70 S6K in hypoxic conditions. Also blocks hypoxia-induced HIF-1α accumulation in a range of human cancer cell lines. Inhibits the expression of HIF target genes, such as carbonic anhydrase IX and MMP2.