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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. GC67941 HIF-PHD-IN-1
  3. GC66464 HIF-1α-IN-2
  4. GC65570 HIF1-IN-3
  5. GC65333 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
  6. GC65133 (S,R,S)-AHPC-C5-COOH
  7. GC65046 M1002
  8. GC64945 M1001 M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM.
  9. GC64584 PHD-1-IN-1 PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM
  10. GC64001 TRC160334
  11. GC63828 Izilendustat
  12. GC63678 HIF-2α-IN-4
  13. GC49190 Roxadustat-d5 An internal standard for the quantification of roxadustat
  14. GC49062 Tiopronin-d3 An internal standard for the quantification of tiopronin
  15. GC62584 HIF-2α-IN-2
  16. GC62418 HIF-2α-IN-3
  17. GC62406 Moracin O
  18. GC62354 Acriflavine hydrochloride
  19. GC62277 AKB-6899
  20. GC61949 1,4-DPCA ethyl ester
  21. GC61863 Verucopeptin
  22. GC61669 Ethyl 3,4-dihydroxybenzoate
  23. GC60919 Hydroxycitric acid tripotassium hydrate
  24. 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。
  25. GC50211 TAT-cyclo-CLLFVY TAT-cyclo-CLLFVY 是 HIF-1 异二聚化的环肽抑制剂,可抑制癌细胞中的缺氧信号传导。 TAT-cyclo-CLLFVY 破坏 HIF-1α/HIF-1β 蛋白质-蛋白质相互作用,IC50 为 1.3 μM。
  26. GC50128 TC-S 7009 An inhibitor of HIF-2α PAS-B domain heterodimerization
  27. GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
  28. GC38767 Deoxyshikonin
  29. GC38044 Fraxinellone A liminoid degradant with diverse biological activities
  30. GC37966 ZINC13466751
  31. GC37889 VCE-004.8
  32. GC37801 TM6089
  33. GC37066 Rac-PT2399
  34. 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).
  35. GC35230 Acetylarenobufagin
  36. GC42785 Amifostine (hydrate) A broad-spectrum radioprotective thiol
  37. GC41625 Oroxylin A A flavonoid with diverse biological activities
  38. GC41572 PRLX-93936 An erastin analog with antitumor activity
  39. GC40918 Gramicidin A A channel-forming ionophore
  40. GC34595 GN44028
  41. GC33634 Enarodustat (JTZ-951) A pan HIF-PH inhibitor
  42. GC33416 AFP464
  43. GC33170 ENMD-119 (ENMD 1198)
  44. GC33043 EL-102
  45. 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.
  46. GC32945 THS-044
  47. GC32876 SYP-5 A HIF-1 inhibitor
  48. GC32724 LW6 (HIF-1α inhibitor) A novel inhibitor of HIF protein accumulation and transcription
  49. GC32680 PT-2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
  50. GC32449 Desidustat An inhibitor of HIF-PH
  51. GC32228 Tilorone dihydrochloride An interferon-inducing antiviral agent

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