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-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
    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-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-N0055R
    Chlorogenic acid (Standard)
    		Inhibitor
    Chlorogenic acid (Standard) is the analytical standard of Chlorogenic acid. This product is intended for research and analytical applications. Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb. It is an orally active antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension compound.
    Chlorogenic acid (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
  • HY-139804
    CTK7A
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer treatment research.
    CTK7A
  • HY-119264
    PRLX-93936
    		Inhibitor
    PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma.
    PRLX-93936
  • HY-158826
    EZN-2968
    EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.
    EZN-2968
  • HY-29090
    ML228 analog
    		Activator
    ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF.
    ML228 analog
  • HY-123009
    KCN1
    		Inhibitor
    KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest.
    KCN1
  • HY-139855
    ZG-2033
    		Agonist
    ZG-2033 (Compound 26) is an orally active HIF-2α agonist that demonstrates nanomolar activity in luciferase reporter gene assays (EC50 = 490 nM). ZG-2033 has the effect of alleviating anemia and exhibits synergistic action with AKB-6548 (HY-101277) in anemia, and can be used in the study of renal anemia.
    ZG-2033
  • HY-13426R
    Roxadustat (Standard)
    		Inhibitor
    Roxadustat (Standard) is the analytical standard of Roxadustat. This product is intended for research and analytical applications. Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.
    Roxadustat (Standard)
  • 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-158826A
    EZN-2968 sodium
    EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.
    EZN-2968 sodium
  • HY-112068
    DM-NOFD
    		Inhibitor
    DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF).
    DM-NOFD
  • HY-114333
    Octyl-α-ketoglutarate
    		Activator
    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-B1080R
    Tilorone (dihydrochloride) (Standard)
    		Activator
    Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS.Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV).
    Tilorone (dihydrochloride) (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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