2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. HIF/HIF Prolyl-Hydroxylase

HIF/HIF Prolyl-Hydroxylase

Hypoxia-inducible factors; HIFs; HIF-PH

HIF/HIF Prolyl-Hydroxylase

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HIFs (Hypoxia-inducible factors) are transcription factors that respond to changes in available oxygen in the cellular environment, to be specific, to decreases in oxygen, or hypoxia. The HIF signaling cascade mediates the effects of hypoxia, the state of low oxygen concentration, on the cell. Hypoxia often keeps cells from differentiating. However, hypoxia promotes the formation of blood vessels, and is important for the formation of a vascular system in embryos, and cancer tumors. The hypoxia in wounds also promotes the migration of keratinocytes and the restoration of the epithelium. In general, HIFs are vital to development. In mammals, deletion of the HIF-1 genes results in perinatal death. HIF-1 has been shown to be vital to chondrocyte survival, allowing the cells to adapt to low-oxygen conditions within the growth plates of bones. HIF plays a central role in the regulation of human metabolism. Recently, several drugs that act as selective HIF prolyl-hydroxylase inhibitors have been developed.

HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

HIF/HIF Prolyl-Hydroxylase Isoform Comparison
Cat. No. 상품명 효과 Purity Chemical Structure
  • HY-77554
    Cephalomannine
    		99.04%
    Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog that can be isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
    Cephalomannine
  • HY-153017
    HIF-1 inhibitor-4
    		Inhibitor 98.11%
    HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
    HIF-1 inhibitor-4
  • HY-100693
    SYP-5
    		Inhibitor 99.21%
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
    SYP-5
  • HY-15672
    FM19G11
    		Inhibitor 98.39%
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
    FM19G11
  • HY-148877
    AT-533
    		Inhibitor 98.38%
    AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs).
    AT-533
  • HY-N3244
    Moracin O
    		Inhibitor 99.98%
    Moracin O is a 2-arylbenzofuran isolated from the Morus alba Linn. . Moracin O exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects.
    Moracin O
  • HY-W613220
    MDH1/2-IN-1
    		Inhibitor 99.53%
    MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 μM and 1.06 μM respectively). MDH1/2-IN-1 inhibits mitochondrial respiration and the HIF-1α pathway. MDH1/2-IN-1 demonstrates significant anti-tumor potential. MDH1/2-IN-1 provides a new direction for the development of drugs targeting cancer metabolism.
    MDH1/2-IN-1
  • HY-114333
    Octyl-α-ketoglutarate
    		Activator 99.9%
    Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD.
    Octyl-α-ketoglutarate
  • HY-115746
    Dimethyl-bisphenol A
    		Inhibitor 99.78%
    Dimethyl-bisphenol A (DMBPA) is a potent HIF-1α inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression.
    Dimethyl-bisphenol A
  • HY-113649
    AKB-6899
    		Inhibitor 99.95%
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
    AKB-6899
  • HY-147025
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
    		Activator 98.62%
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used for research on prostate cancer and other cancers.
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
  • HY-123422
    GSK360A
    		Inhibitor 99.90%
    GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
    GSK360A
  • HY-159120
    ZG-2291
    		Inhibitor 98.08%
    ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases.
    ZG-2291
  • HY-N0487
    Glucosamine sulfate
    		Inhibitor 98.0%
    Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine sulfate
  • HY-146144
    HIF-IN-1
    		Inhibitor 98.00%
    HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity.
    HIF-IN-1
  • HY-19621
    THS-044
    		Modulator 99.67%
    THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (KD = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia.
    THS-044
  • HY-153016
    HIF-2α agonist 2
    		Agonist 99.59%
    HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research.
    HIF-2α agonist 2
  • HY-15893R
    DMOG (Standard)
    		Inhibitor
    DMOG (Standard) is the analytical standard of DMOG. This product is intended for research and analytical applications. DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
    DMOG (Standard)
  • HY-111547
    M1001
    		Agonist 99.51%
    M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.
    M1001
  • HY-N3243
    Moracin P
    		Inhibitor 99.62%
    Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects.
    Moracin P
Cat. No. 상품명 / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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