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-N6031
    Dendrophenol
    		Inhibitor 99.93%
    Dendrophenol (Moscatilin) is a NF-κB inhibitor that inhibits inflammation. Dendrophenol exerts potent cytotoxic effect against tumor cells and induces cell cycle arrest and apoptosis. Dendrophenol has antitumor activity. In addition, Dendrophenol can inhibit vascular calcification by inhibiting the activation of WNT3/β-catenin.
    Dendrophenol
  • HY-N5112A
    β,β-Dimethylacrylalkannin
    		99.36%
    β,β-Dimethylacrylalkannin (Arnebin 1) is a napthoquinone isolated from Alkanna cappadocica , increases collagen and involucrin content in skin cells.
    β,β-Dimethylacrylalkannin
  • HY-112144
    TP0463518
    		Inhibitor 99.25%
    TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM.
    TP0463518
  • HY-100693
    SYP-5
    		Inhibitor 99.21%
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
    SYP-5
  • 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-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-N0733
    Glucosamine hydrochloride
    		Inhibitor ≥98.0%
    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 dietary supplement. Glucosamine hydrochloride 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 hydrochloride
  • HY-N0910
    Notoginsenoside Ft1
    		≥98.0%
    Notoginsenoside Ft1 is a saponin isolated from Panax notoginseng; stimulator of angiogenesis.
    Notoginsenoside Ft1
  • HY-101449
    Adaptaquin
    		Inhibitor 99.87%
    Adaptaquin is a BBB-penatrable HIF-PHDs inhibitor. Adaptaquin has anti-inflammatory and neuroprotective effects. Adaptaquin can effectively inhibit lipid peroxidation, maintain mitochondrial function, and reduce neuronal death. Adaptaquin can be used in the research of nervous system diseases such as Parkinson's disease.
    Adaptaquin
  • HY-P1420
    TAT-cyclo-CLLFVY
    		Inhibitor
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
    TAT-cyclo-CLLFVY
  • HY-P2324
    Gramicidin A
    		Inhibitor 98.10%
    Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
    Gramicidin A
  • HY-147025
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
    		Activator 99.06%
    (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
  • HY-115903
    HIF-1α-IN-2
    		Inhibitor 98.45%
    HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
    HIF-1α-IN-2
  • HY-120087
    KG-548
    		Inhibitor 99.92%
    KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
    KG-548
  • HY-B1295
    Lithium citrate tetrahydrate
    		Inhibitor ≥98.0%
    Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
    Lithium citrate tetrahydrate
  • HY-P2657
    Verucopeptin
    		Inhibitor ≥99.0%
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
    Verucopeptin
  • 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-124586
    Streptonigrin
    		Inhibitor 99.20%
    Streptonigrin (Bruneomycin) is an orally active antibiotic and pan-PAD inhibitor, inhibiting PAD1, PAD2, PAD3 and PAD4 with IC50 of 48.3 μM, 26.1 μM, 0.43 μM and 2.5 μM, respectively. Streptonigrin inhibits SENP1 (IC50 of 0.518 μM) and reduces HIF1α. Streptonigrin increases p53 and Apoptosis. Streptonigrin shows antiviral activity against Rauscher murine leukemia virus. Streptonigrin has immunosuppressive effects. Streptonigrin has antitumor activity against osteosarcoma.
    Streptonigrin
  • HY-N1477
    Dencichine
    		Inhibitor 99.59%
    Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
    Dencichine
  • HY-77554
    Cephalomannine
    		98.49%
    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
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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