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
- Cat.No. 产品名称 Information
- 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。
- GC50128 TC-S 7009 An inhibitor of HIF-2α PAS-B domain heterodimerization
- GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
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GC38767
Deoxyshikonin
去氧紫草素
Deoxyshikonin 是从 Lithospermum erythrorhizon Sieb 中分离得到的,具有抗肿瘤活性。 -
GC38044
Fraxinellone
梣酮
A liminoid degradant with diverse biological activities - 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。
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GC37889
VCE-004.8
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。 - 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。
- 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。
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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). -
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。 -
GC41625
Oroxylin A
千层纸素A; Baicalein 6-methyl ether; 6-Methoxybaicalein
A flavonoid with diverse biological activities - 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。
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GC33634
Enarodustat (JTZ-951)
JTZ-951
A pan HIF-PH inhibitor -
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。 -
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。 - 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。
- 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.
- GC32945 THS-044 THS-044结合且稳定化HIF2αPAS-B折叠状态,调节HIF2活性。
- GC32876 SYP-5 A HIF-1 inhibitor
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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。 - GC32680 PT-2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
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GC32449
Desidustat
ZYAN1
An inhibitor of HIF-PH -
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 -
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。 - GC31498 TP0463518 A pan HIF-PH inhibitor
- GC31358 HIF-2α-IN-1 HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。
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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。 -
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. - GC19251 MK-8617 A HIF-PH1, -2, and -3 inhibitor
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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 -
GC16811
Vadadustat
伐度司他,PG-1016548; AKB-6548
An inhibitor of HIF-PH2 and HIF-PH3 -
GC16195
2,4-DPD
2,4-吡啶二甲酸乙酯,2,4-Diethylpyridine dicarboxylate
A cell permeable, competitive inhibitor of HIF-PH -
GC15379
JNJ-42041935
HIF-PHD Inhibitor II
A selective inhibitor of HIF-PH enzymes - GC12255 IOX4 A selective, bioavailable inhibitor of HIF-PH2
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GC12487
Adaptaquin
HIF prolyl hydroxylase inhibitor
An inhibitor of HIF-PH2 -
GC17358
Octyl-α-ketoglutarate
α-KG octyl ester
A cell-permeable form of α-ketoglutarate -
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 -
GC16647
Daprodustat(GSK1278863)
达普司他,GSK1278863
A HIF-PH1, -2, and -3 inhibitor - 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。
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GC12821
Oltipraz
奥替普拉; RP 35972; NSC 347901
A Nrf2 and CAR activator -
GC10046
Molidustat (BAY85-3934)
BAY 85-3934
A pan-HIF-PH inhibitor -
GC16638
FG2216
IOX3; YM311
An inhibitor of HIF-PH2 -
GC11767
Hydralazine HCl
盐酸肼屈嗪
An antihypertensive agent - GC12698 BAY 87-2243 A mitochondrial complex I inhibitor and inducer of ferroptosis
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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。 -
GC15594
PX 12
2-(仲丁基二硫基)-1H-咪唑,IV-2
An irreversible inhibitor of thioredoxin-1 -
GC14319
ML 228
CID-46742353
A HIF pathway activator - GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis
- GC13018 IOX2(Glycine) A selective PHD2 inhibitor