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. Product Name Effect Purity Chemical Structure
  • HY-112678
    TM6008
    		Inhibitor 99.51%
    TM6008 is a potent and orally active prolyl hydroxylase (PHD) inhibitor. TM6008 chelats transition metal (copper) and inhibits the autoxidation of ascorbic acid with an IC50 value is 0.57 μM. TM6008  exerts organ protection against ischemia in vivo and can be used for cerebrovascular disease research.
    TM6008
  • 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-B0413R
    Fenbendazole (Standard)
    		Activator
    Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53.
    Fenbendazole (Standard)
  • HY-B0223R
    Albendazole (Standard)
    		Inhibitor
    Albendazole (Standard) is the analytical standard of Albendazole. This product is intended for research and analytical applications. Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells.
    Albendazole (Standard)
  • HY-W654013
    Minocycline-d7
    		Inhibitor
    Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
    Minocycline-d<sub>7</sub>
  • HY-151341
    HIF-1/2α-IN-1
    		Inhibitor
    HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
    HIF-1/2α-IN-1
  • HY-148264
    Imdatifan
    		Inhibitor
    Imdatifan (HIF-2α-IN-7) is a hypoxia inducible factor 2α (HIF-2α) inhibitor. Imdatifan can inhibit HIF-2α with an EC50 value of 6 nM. Imdatifan can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders.
    Imdatifan
  • HY-109057A
    Enarodustat hydrochloride
    		Inhibitor
    Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.
    Enarodustat hydrochloride
  • HY-44809A
    Izilendustat hydrochloride
    		Inhibitor
    Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
    Izilendustat hydrochloride
  • HY-144178
    HIF-2α-IN-6
    		Inhibitor
    HIF-2α-IN-6 (117) is a HIF-2α inhibitor.
    HIF-2α-IN-6
  • HY-112441
    Prolyl Hydroxylase inhibitor 1
    		Inhibitor
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
    Prolyl Hydroxylase inhibitor 1
  • HY-N0560R
    Oroxylin A (Standard)
    		Inhibitor
    Oroxylin A (Standard) is the analytical standard of Oroxylin A. This product is intended for research and analytical applications. Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis.
    Oroxylin A (Standard)
  • HY-169100
    Antiproliferative agent-57
    		Inhibitor
    Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.
    Antiproliferative agent-57
  • HY-141510A
    myo-Inositol trispyrophosphate hexa-triethylamine
    		98.0%
    myo-Inositol trispyrophosphate (ITPP) hexa-triethylamine is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate hexa-triethylamine is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate hexa-triethylamine enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate hexa-triethylamine can be used in the study of cardiovascular disease and cancer.
    myo-Inositol trispyrophosphate hexa-triethylamine
  • HY-N0596R
    Panaxadiol (Standard)
    		Inhibitor
    Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
    Panaxadiol (Standard)
  • HY-161586
    Chloramphenicol/BSA
    		Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-161265
    HIF-2α agonist 3
    		Agonist
    HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with a EC50 value of 1.78 μM. HIF-2α agonist 3 can be used in the study of renal anemia.
    HIF-2α agonist 3
  • HY-P1888A
    HIF-1 alpha (556-574) TFA
    HIF-1 alpha (556-574) TFA is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis.
    HIF-1 alpha (556-574) TFA
  • HY-18259
    103D5R
    		Inhibitor
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM.
    103D5R
  • HY-170027
    LW1564
    		Inhibitor
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.
    LW1564
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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