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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. Cat.No. Product Name Information
  2. C4887 2,4-DPD cell permeable, competitive inhibitor of HIF-PH
  3. A4188 2-Methoxyestradiol (2-MeOE2) Apoptotic, antiproliferative and antiangiogenic agent
  4. C4377 Adaptaquin HIF-prolyl hydroxylase-2 (PHD2) inhibitor
  5. B1115 BAY 87-2243 HIF-1 inhibitor,potent and selective
  6. B6106 Daprodustat(GSK1278863) HIF-prolyl hydroxylase inhibitor
  7. A4506 DMOG Competitive HIF-PH inhibitor, cell-permeable
  8. A4187 FG-4592 (ASP1517) HIF prolyl-hydroxylase inhibitor
  9. B5851 FG2216 HIF-prolyl hydroxylase inhibitor
  10. A4189 IOX2(Glycine) HIF-1α prolyl hydroxylase-2 (PHD2) inhibitor
  11. C4752 JNJ-42041935 Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor

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