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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.

  1. Cat.No. 产品名称 Information
  2. GC50537 FM19G11 FM19G11 是一种低氧诱导因子-1-α (HIF-1α) 抑制剂,在 HeLa 细胞中抑制低氧诱导的荧光素酶活性,IC50 为 80 nM。
  3. GC50128 TC-S 7009 An inhibitor of HIF-2α PAS-B domain heterodimerization
  4. GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
  5. GC38767 Deoxyshikonin
  6. GC38044 Fraxinellone A liminoid degradant with diverse biological activities
  7. GC37966 ZINC13466751
  8. GC37889 VCE-004.8
  9. GC37801 TM6089
  10. GC37066 Rac-PT2399
  11. GC37034 PT2977 PT2977 (Belzutifan, MK-6482), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).
  12. GC35230 Acetylarenobufagin
  13. GC41625 Oroxylin A A flavonoid with diverse biological activities
  14. GC34595 GN44028
  15. GC33634 Enarodustat (JTZ-951) A pan HIF-PH inhibitor
  16. GC33416 AFP464
  17. GC33170 ENMD-119 (ENMD 1198)
  18. GC33043 EL-102
  19. GC32948 IDF-11774 IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells.
  20. GC32945 THS-044
  21. GC32876 SYP-5 A HIF-1 inhibitor
  22. GC32724 LW6 (HIF-1α inhibitor)

    LW6 is a hypoxia-inducing factor 1(HIF) inhibitor, which effectively inhibits HIF-1α accumulation by degrading HIF-1α, but does not affect HIF-1A mRNA level during hypoxia.

  23. GC32680 PT-2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
  24. GC32449 Desidustat An inhibitor of HIF-PH
  25. GC32228 Tilorone dihydrochloride An interferon-inducing antiviral agent
  26. GC32083 Acriflavine
  27. GC31498 TP0463518 A pan HIF-PH inhibitor
  28. GC31358 HIF-2α-IN-1
  29. GC31230 Dencichin (Dencichine)
  30. GC30263 Glucosamine (D-Glucosamine) Glucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. Glucosamine(GS) treatment selectively downregulates HIF-1α at the protein level in YD-8 cells via interference of production of the citric acid cycle metabolites.
  31. GC19251 MK-8617 A HIF-PH1, -2, and -3 inhibitor
  32. GC18236 Echinomycin An inhibitor of HIF-1-mediated gene transcription
  33. GC16811 Vadadustat An inhibitor of HIF-PH2 and HIF-PH3
  34. GC16195 2,4-DPD A cell permeable, competitive inhibitor of HIF-PH
  35. GC15379 JNJ-42041935 A selective inhibitor of HIF-PH enzymes
  36. GC12255 IOX4 A selective, bioavailable inhibitor of HIF-PH2
  37. GC12487 Adaptaquin An inhibitor of HIF-PH2
  38. GC17358 Octyl-α-ketoglutarate A cell-permeable form of α-ketoglutarate
  39. GC14282 3-acetyl-11-keto-β-Boswellic Acid A selective 5-LO inhibitor
  40. GC16647 Daprodustat(GSK1278863) A HIF-PH1, -2, and -3 inhibitor
  41. GC11031 PX-478 2HCl Suppressor of HIF-1α levels in cancer cells
  42. GC12821 Oltipraz A Nrf2 and CAR activator
  43. GC10046 Molidustat (BAY85-3934) A pan-HIF-PH inhibitor
  44. GC16638 FG2216 An inhibitor of HIF-PH2
  45. GC11767 Hydralazine HCl An antihypertensive agent
  46. GC12698 BAY 87-2243 A mitochondrial complex I inhibitor and inducer of ferroptosis
  47. GC16973 DMOG An HIF-PH inhibitor
  48. GC15594 PX 12 An irreversible inhibitor of thioredoxin-1
  49. GC14319 ML 228 A HIF pathway activator
  50. GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis
  51. GC13018 IOX2(Glycine) A selective PHD2 inhibitor

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