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-N14331
    Fibrostatin B
    		Inhibitor
    Fibrostatin B is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin B
  • HY-12654R
    Molidustat (Standard)
    		Inhibitor
    Molidustat (Standard) is the analytical standard of Molidustat. This product is intended for research and analytical applications. Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia.
    Molidustat (Standard)
  • HY-103227R
    Desidustat (Standard)
    		Inhibitor
    Desidustat (Standard) is the analytical standard of Desidustat. This product is intended for research and analytical applications. Desidustat is an orally active HIF hydroxylase inhibitor. Desidustat can be used for the research of various disorders including anemia of different types and conditions associated with ischemia/hypoxia.
    Desidustat (Standard)
  • 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)
  • HY-12519R
    Oltipraz (Standard)
    		Inhibitor
    Oltipraz (Standard) is the analytical standard of Oltipraz. This product is intended for research and analytical applications. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz (Standard)
  • HY-D2360
    O-Carboranylphenoxyacetanilide
    		Inhibitor
    O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity.
    O-Carboranylphenoxyacetanilide
  • HY-B1125S
    Glucosamine-13C6
    		Inhibitor
    Glucosamine-13C6 (D-Glucosamine-13C6) is 13C labeled Glucosamine. Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine 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-<sup>13</sup>C<sub>6</sub>
  • HY-15692
    PHD2-IN-3
    		Inhibitor
    PHD2-IN-3 (compound 2) is a PHD2 inhibitor. PHD2-IN-3 can be used for study of anemia.
    PHD2-IN-3
  • HY-17608R
    Daprodustat (Standard)
    		Inhibitor
    Daprodustat (Standard) is the analytical standard of Daprodustat. This product is intended for research and analytical applications. Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
    Daprodustat (Standard)
  • HY-N0787R
    Cryptochlorogenic acid (Standard)
    		Inhibitor
    Cryptochlorogenic acid (Standard) is the analytical standard of Cryptochlorogenic acid. This product is intended for research and analytical applications. Cryptochlorogenic acid is a natural product.
    Cryptochlorogenic acid (Standard)
  • HY-17617R
    Nastorazepide (Standard)
    		Inhibitor
    Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide (Standard)
  • HY-12315R
    N-Oxalylglycine (Standard)
    		Inhibitor
    N-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively.
    N-Oxalylglycine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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