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-B1625R
    Deferoxamine (Standard)
    		Activator
    Deferoxamine (Standard) is the analytical standard of Deferoxamine. This product is intended for research and analytical applications. Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
    Deferoxamine (Standard)
  • HY-N6030
    (Rac)-Dencichine
    (Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
    (Rac)-Dencichine
  • HY-W747868
    Molidustat sodium
    		Inhibitor
    Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia.
    Molidustat sodium
  • HY-P5915
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2
    		Agonist
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2, a 5-FAM labeled HIF-1α peptide, is a substrate of VHL. FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2 binds to VHL protein with a KD of 3 nM. Ex/Em (λ) = 485/520 nm.
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2
  • HY-147426
    Zifcasiran
    		Inhibitor
    Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.
    Zifcasiran
  • HY-N6905
    Acetylarenobufagin
    		Modulator
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
    Acetylarenobufagin
  • HY-146540
    GEM-5
    		Inhibitor
    GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
    GEM-5
  • HY-17412AS
    Minocycline-d6
    		Inhibitor
    Minocycline-d6 is deuterium labeled Minocycline (HY-17412A). 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>6</sub>
  • HY-163603
    HIF-2α-IN-16
    		Inhibitor
    HIF-2α-IN-16 (48) is a HIF-2α inhibitor, with an IC50 of 0.091 μM.
    HIF-2α-IN-16
  • HY-144176
    HIF-2α-IN-5
    		Inhibitor
    HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.
    HIF-2α-IN-5
  • HY-156527
    PHD-IN-2
    		Inhibitor
    PHD-IN-2 (Compound 91) is a PHD antagonist (IC50: < 5 nM). PHD-IN-2 induces erythropoietin synthesis in HEP3B cells (EC50: <2.5 μM). PHD-IN-2 can be used for research of cardiovascular disorders, metabolic disorders, hematological disorders, pulmonary disorders, kidney disorders, liver disorders, wound healing disorders, and cancer.
    PHD-IN-2
  • HY-163370
    HIF-1α-IN-7
    		Inhibitor
    HIF-1α-IN-7 (Compound D13) is a potent HIF-1α inhibitor. HIF-1α-IN-7 has neuroprotective activity. HIF-1α-IN-7 can be used in Alzheimer's disease research.
    HIF-1α-IN-7
  • 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-162438
    PHD2-IN-2
    		Inhibitor
    PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia.
    PHD2-IN-2
  • HY-N0733S
    Glucosamine-13C hydrochloride
    Glucosamine-13C (hydrochloride) is the 13C labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a
    Glucosamine-<sup>13</sup>C hydrochloride
  • HY-149886
    HIF-2α-IN-9
    		Inhibitor
    HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity.
    HIF-2α-IN-9
  • HY-176408
    PHD2-IN-5
    		Inhibitor
    PHD2-IN-5 (compound 22) is a potent PHD2 inhibitor with an IC50 of 0.82 μM. PHD2-IN-5 can be used in the study of renal anemia.
    PHD2-IN-5
  • HY-N0265R
    Asperosaponin VI (Standard)
    Asperosaponin VI (Standard) is the analytical standard of Asperosaponin VI. This product is intended for research and analytical applications. Asperosaponin VI is a saponin component from Dipsacus asper. Asperosaponin VI induces osteoblast differentiation through the BMP-2/p38 and ERK1/2 signaling pathways. Asperosaponin VI protects against hypoxia-induced cardiomyocyte apoptosis by activating the PI3K/Akt and CREB pathways. Additionally, Asperosaponin VI also has antidepressant and wound-healing-promoting activities.
    Asperosaponin VI (Standard)
  • 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-113662
    CLB-016
    		Inhibitor
    CLB-016 is a potent Hypoxia-inducible factor (HIF-1) inhibitor with an IC50 of 19.1 μM. CLB-016 significantly suppresses HIF-1-mediated hypoxia response.
    CLB-016
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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