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-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-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-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-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-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-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
  • 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-101277S1
    Vadadustat-13C6
    		Inhibitor
    Vadadustat-13C6 (PG-1016548-13C6) is 13C labeled Vadadustat. Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
    Vadadustat-<sup>13</sup>C<sub>6</sub>
  • 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-N14330
    Fibrostatin A
    		Inhibitor
    Fibrostatin A is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin A
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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