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Home >> Signaling Pathways >> Angiogenesis >> HIF

HIF(缺氧诱发因素)

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 Deoxyshikonin 是从 Lithospermum erythrorhizon Sieb 中分离得到的，具有抗肿瘤活性。
  6. GC38044 Fraxinellone A liminoid degradant with diverse biological activities
  7. GC37966 ZINC13466751 ZINC13466751 是一种 HIF-1α/von Hippel-Lindau 相互作用的有效抑制剂，IC50 值为 2.0 ?M。
  8. GC37889 VCE-004.8 VCE-004.8 (VCE-004.8) 是一种具有口服活性的特异性 PPARγ；和 CB2 受体双重激动剂。
  9. GC37801 TM6089 TM6089 是一种独特的 PHD 抑制剂，可刺激 HIF 活性而不会产生铁螯合作用，诱导血管生成并对缺血器官发挥保护作用。 TM6089 局部施用可增强血管生成，并且口服施用在表达缺氧反应的报告载体的转基因大鼠中刺激 HIF 活性。
  10. GC37066 Rac-PT2399 Rac-PT2399 (Compound 10e) 是 PT2399 的消旋体，是一种有效且特异性的缺氧诱导因子 2a (HIF-2α) 抑制剂，IC50 为 0.01 μM。
  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 Acetylarenobufagin 是一种类固醇缺氧诱导因子-1 (HIF-I) 调节剂。
  13. GC41625 Oroxylin A A flavonoid with diverse biological activities
  14. GC34595 GN44028 GN44028 是一种有效且具有口服活性的缺氧诱导因子 (HIF)-1α 抑制剂，IC50 为 14 nM。 GN44028 抑制缺氧诱导的 HIF-1α 转录活性，而不抑制 HIF-1α mRNA 表达、HIF-1α 蛋白积累或 HIF-1α/HIF-1β 异二聚化。 GN44028可用于癌症研究。
  15. GC33634 Enarodustat (JTZ-951) A pan HIF-PH inhibitor
  16. GC33416 AFP464 AFP464（NSC710464 游离碱基），是一个活跃的 HIF-1α；抑制剂，IC50 为 0.25 μM，也是一种有效的芳烃受体 (AhR) 激活剂。
  17. GC33170 ENMD-119 (ENMD 1198) ENMD-119 (ENMD 1198) (IRC-110160) 是一种口服活性微管去稳定剂，是一种具有抗增殖和抗血管生成活性的 2-甲氧基雌二醇类似物。 ENMD-119 (ENMD 1198) 适用于抑制人类 HCC 细胞中的 HIF-1alpha 和 STAT3，并导致肿瘤生长和血管形成减少。
  18. GC33043 EL-102 EL102是HIF1α的抑制剂，能够抑制微管蛋白聚合和减少它的稳定性。
  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 THS-044结合且稳定化HIF2αPAS-B折叠状态,调节HIF2活性。
  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 Acriflavine是用于标记高分子量RNA的荧光染料。它也是一种局部防腐剂。
  27. GC31498 TP0463518 A pan HIF-PH inhibitor
  28. GC31358 HIF-2α-IN-1 HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。
  29. GC31230 Dencichin (Dencichine) Dencichin是一种最初从三七中提取的非蛋白质氨基酸，可以抑制HIF-脯氨酰羟化酶2（PHD-2）的活性。
  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

    PX-478是一种选择性抑制剂，可以抑制常规和低氧诱导的HIF-1α水平
  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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