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-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-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-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
  • 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-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-N14340
    Fibrostatin F
    		Inhibitor
    Fibrostatin F is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin F
  • HY-29090
    ML228 analog
    		Activator
    ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF.
    ML228 analog
  • HY-N0487R
    Glucosamine sulfate (Standard)
    		Inhibitor
    Glucosamine (sulfate) (Standard) is the analytical standard of Glucosamine (sulfate). This product is intended for research and analytical applications. Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate 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 sulfate (Standard)
  • HY-N2518R
    Agnuside (Standard)
    		Inhibitor
    Agnuside (Standard) is the analytical standard of Agnuside. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N14332
    Fibrostatin D
    		Inhibitor
    Fibrostatin D is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin D
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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