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Home >> Signaling Pathways >> Chromatin/Epigenetics >> 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.

Products for  HIF

  1. Cat.No. 产品名称 Information
  2. 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。
  3. 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。
  4. GC37034 PT2977

    PT2977; MK-6482

     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).
  5. GC35230 Acetylarenobufagin

    乙酰沙蟾毒精

     Acetylarenobufagin 是一种类固醇缺氧诱导因子-1 (HIF-I) 调节剂。
  6. GC42785 Amifostine (hydrate)

    氨磷汀三水合物,WR2721 trihydrate

     A broad-spectrum radioprotective thiol
  7. GC41625 Oroxylin A

    千层纸素A; Baicalein 6-methyl ether; 6-Methoxybaicalein

     A flavonoid with diverse biological activities
  8. GC41572 PRLX-93936 An erastin analog with antitumor activity
  9. GC40918 Gramicidin A

    甲胎蛋白

     A channel-forming ionophore
  10. GC40555 Tiopronin

    BRN 1859822, (±)-Tiopronin

     Tiopronin is an antioxidant that has diverse biological activities.
  11. 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。
  12. GC33634 Enarodustat (JTZ-951)

    JTZ-951

     A pan HIF-PH inhibitor
  13. GC33416 AFP464

    NSC710464 free base

     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。
  14. GC33170 ENMD-119 (ENMD 1198)

    IRC-110160

     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。
  15. 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。
  16. 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.
  17. GC32945 THS-044 THS-044结合且稳定化HIF2αPAS-B折叠状态,调节HIF2活性。
  18. GC32876 SYP-5 A HIF-1 inhibitor
  19. GC32724 LW6 (HIF-1α inhibitor)

    HIF-1α inhibitor; LW8

     LW6是一种缺氧诱导因子1(hypoxia inducing factor 1, HIF)抑制剂,通过降解HIF-1α有效抑制HIF-1α的积累,但不影响缺氧时HIF- 1a mRNA水平。
  20. GC32680 PT-2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
  21. GC32449 Desidustat

    ZYAN1

     An inhibitor of HIF-PH
  22. GC32228 Tilorone dihydrochloride

    盐酸替洛隆；梯洛龙二盐酸盐；替洛隆二盐酸盐；盐酸梯洛龙

     An interferon-inducing antiviral agent
  23. GC32083 Acriflavine

    吖啶黄; Acriflavinium chloride 3,6-Acridinediamine mix

     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。
  24. GC31498 TP0463518 A pan HIF-PH inhibitor
  25. GC31358 HIF-2α-IN-1 HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。
  26. GC31230 Dencichin (Dencichine)

    三七素; Dencichin; ODAP

     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。
  27. GC30263 Glucosamine (D-Glucosamine)

    氨基葡萄糖; D-Glucosamine; Chitosamine

     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.
  28. GC19251 MK-8617 A HIF-PH1, -2, and -3 inhibitor
  29. GC18236 Echinomycin

    醌霉素A,Antibiotic A 654I； NSC 13502； NSC 526417； Quinomycin A； SK 302B

     An inhibitor of HIF-1-mediated gene transcription
  30. GC16811 Vadadustat

    伐度司他,PG-1016548; AKB-6548

     An inhibitor of HIF-PH2 and HIF-PH3
  31. GC15379 JNJ-42041935

    HIF-PHD Inhibitor II

     A selective inhibitor of HIF-PH enzymes
  32. GC12255 IOX4 A selective, bioavailable inhibitor of HIF-PH2
  33. GC14282 3-acetyl-11-keto-β-Boswellic Acid

    11-羰基-Β-乙酰乳香酸,3-O-acetyl-11-keto-β-Boswellic acid,AKBA

     A selective 5-LO inhibitor
  34. GC16647 Daprodustat(GSK1278863)

    达普司他,GSK1278863

     A HIF-PH1, -2, and -3 inhibitor
  35. 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。
  36. GC12821 Oltipraz

    奥替普拉; RP 35972; NSC 347901

     A Nrf2 and CAR activator
  37. GC10046 Molidustat (BAY85-3934)

    BAY 85-3934

     A pan-HIF-PH inhibitor
  38. GC16638 FG2216

    IOX3; YM311

     An inhibitor of HIF-PH2
  39. GC11767 Hydralazine HCl

    盐酸肼屈嗪

     An antihypertensive agent
  40. GC12698 BAY 87-2243 A mitochondrial complex I inhibitor and inducer of ferroptosis
  41. GC16973 DMOG

    二甲基乙二酰氨基乙酸,Dimethyloxallyl Glycine

     DMOG（二羟基丙氨酸）是 α-酮戊二酸辅助因子的拮抗剂和 HIF-脯氨酸羟化酶的抑制剂，导致 HIF-1α 蛋白在细胞核中的稳定和积累。
  42. GC15594 PX 12

    2-(仲丁基二硫基)-1H-咪唑,IV-2

     An irreversible inhibitor of thioredoxin-1
  43. GC14319 ML 228

    CID-46742353

     A HIF pathway activator
  44. GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis
  45. GC17405 Chetomin

    毛壳菌素,NSC 289491

     An inhibitor of HIF signaling
  46. GC13018 IOX2(Glycine) A selective PHD2 inhibitor
  47. GC15084 2-Methoxyestradiol (2-MeOE2)

    二甲氧基雌二醇; 2-ME2; NSC-659853

     2-Methoxyestradiol (2-MeOE2/2-Me)是一种HIF-1α抑制剂。
  48. GC13139 FG-4592 (ASP1517)

    罗沙司他,Roxadustat

     FG-4592 作为一种口服生物可利用的缺氧诱导因子 (HIF) 脯氨酰羟化酶抑制剂，可通过 HIF 介导的转录促进协调性红细胞生成。
  49. GN10518 Chitosamine hydrochloride

    盐酸氨基葡萄糖; D-(+)-Glucosamine hydrochloride; Chitosamine hydrochloride

     An amino monosaccharide
  50. GN10669 Glucosamine sulfate

    硫酸氨基葡萄糖; D-Glucosamine sulfate

     氨基葡萄糖硫酸盐（D-氨基葡萄糖硫酸盐）是一种氨基糖，是糖基化蛋白质和脂质生化合成的重要前体，用作膳食补充剂。
  51. GN10308 Chlorogenic acid

    绿原酸; 3-O-Caffeoylquinic acid; Heriguard; NSC-407296

     Chlorogenic acid是一种有效的神经保护剂，同时具有抗病毒、抗真菌、抗氧化和抗肿瘤作用。Chlorogenic acid还参与调节葡萄糖和脂质代谢，改善胰岛素敏感性。

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