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-N2518
    Agnuside
    		Inhibitor 99.90%
    Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.
    Agnuside
  • HY-141510
    myo-Inositol trispyrophosphate hexasodium
    		≥98.0%
    myo-Inositol trispyrophosphate (ITPP) hexasodium is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate (ITPP) hexasodium is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate (ITPP) hexasodium enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate (ITPP) hexasodium can be used in the study of cardiovascular disease and cancer.
    myo-Inositol trispyrophosphate hexasodium
  • HY-153016
    HIF-2α agonist 2
    		Agonist 99.63%
    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-44809
    Izilendustat
    		Inhibitor 99.20%
    Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
    Izilendustat
  • HY-136748
    HIF-2α-IN-4
    		Inhibitor 99.96%
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
    HIF-2α-IN-4
  • HY-124473
    Naphthofluorescein
    		Inhibitor 99.52%
    Naphthofluorescein inhibits the interaction between HIF-1 and Mint3. Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging.
    Naphthofluorescein
  • HY-148877
    AT-533
    		Inhibitor 98.86%
    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-N5112B
    β,β-Dimethylacrylshikonin
    		99.30%
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Lithospermum erythrorhizon Sieb. et Zucc. , promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
    β,β-Dimethylacrylshikonin
  • HY-151344
    HIF-1/2α-IN-2
    		Inhibitor 99.55%
    HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).
    HIF-1/2α-IN-2
  • HY-B0639A
    Amifostine trihydrate
    		Activator 99.95%
    Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action.
    Amifostine trihydrate
  • HY-158341
    IOX5
    		Inhibitor 99.39%
    IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity.
    IOX5
  • HY-108868
    Mersalyl
    		Inducer
    Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.
    Mersalyl
  • 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-N5112
    (Rac)-Arnebin 1
    		99.36%
    (Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity.
    (Rac)-Arnebin 1
  • HY-132989
    Mal-Deferoxamine
    		Activator
    Mal-Deferoxamine is a maleamide (Mal)-containing Deferoxamine (HY-B1625). Mal selectively covalently binds to sulfur groups to produce a linking reaction. Mal-Deferoxamine can be combined with radionuclides to synthesize radionuclide drug conjugates (RDCs). RDCs have the ability to specifically target biomolecules and can be used in medical imaging or therapy..
    Mal-Deferoxamine
  • HY-B2141
    Bendazol
    		Inhibitor 99.78%
    Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats.
    Bendazol
  • HY-119264A
    PRLX-93936 dihydrochloride
    		Inhibitor 99.83%
    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 dihydrochloride
  • HY-16187
    EL-102
    		Inhibitor 99.44%
    EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
    EL-102
  • HY-108697A
    (Rac)-PT2399
    		Inhibitor 99.84%
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
    (Rac)-PT2399
  • HY-142693
    Angiogenesis agent 1
    		Activator 99.39%
    Angiogenesis agent 1 (compound C-31) is a salidroside-derivated glycoside analogue. Angiogenesis agent 1 is an activator of the HIF-1α pathway. Angiogenesis agent 1 has the potential for the research of diabetic hind limb ischemia.
    Angiogenesis agent 1
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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