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HIF

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.

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  1. 2,4-DPD
    Catalog No. :
    C4887
    cell permeable, competitive inhibitor of HIF-PH
  2. JNJ-42041935
    Catalog No. :
    C4752
    Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor
  3. Adaptaquin
    Catalog No. :
    C4377
    HIF-prolyl hydroxylase-2 (PHD2) inhibitor
  4. Octyl-α-ketoglutarate
    Catalog No. :
    C4321
    prolyl hydroxylases (PHD) activator
  5. Daprodustat(GSK1278863)
    Catalog No. :
    B6106
    HIF-prolyl hydroxylase inhibitor
  6. FG2216
    Catalog No. :
    B5851
    HIF-prolyl hydroxylase inhibitor
    FG-2216 is a potent HIF-prolyl hydroxylase inhibitor. IC50 = 3.9 μM for PDH2 enzyme.
  7. BAY 87-2243
    Catalog No. :
    B1115
    HIF-1 inhibitor,potent and selective
    BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation .
  8. DMOG
    Catalog No. :
    A4506
    Competitive HIF-PH inhibitor, cell-permeable
    Prolyl 4-hydroxylase (P4H) inhibitor; inhibits hypoxia-inducible factor α (HIF-α) prolyl hydroxylase (HIF-PH).
  9. PX 12
    Catalog No. :
    A4509
    Trx-1 inhibitor
    Competitive, 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.
  10. KC7F2
    Catalog No. :
    A4507
    HIF-1α inhibitor
    Inhibitor 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.

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