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-180560
    PHD-IN-5
    		Inhibitor
    PHD-IN-5 (ISM4808) is an orally active PHD inhibitor that can be used for studying anemia in chronic kidney disease.
    PHD-IN-5
  • 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-153512
    PHD-1-IN-3
    		Inhibitor
    PHD-1-IN-3 is an orally active PHD-1 inhibitor with an IC50 of 0.09 μM. PHD-1-IN-3 acts via monodentate binding interaction with active site Fe2+ ion.
    PHD-1-IN-3
  • HY-N14330
    Fibrostatin A
    		Inhibitor
    Fibrostatin A is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin A
  • HY-108697AR
    (Rac)-PT2399 (Standard)
    		Inhibitor
    (Rac)-PT2399 (Standard) is the analytical standard of (Rac)-PT2399 (HY-108697A). This product is intended for research and analytical applications. (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 (Standard)
  • HY-100693R
    SYP-5 (Standard)
    		Inhibitor
    SYP-5 (Standard) is the analytical standard of SYP-5 (HY-100693). This product is intended for research and analytical applications. SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
    SYP-5 (Standard)
  • HY-N14339
    Fibrostatin E
    		Inhibitor
    Fibrostatin E is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin E
  • HY-15641R
    FG-2216 (Standard)
    		Inhibitor
    FG-2216 (Standard) is the analytical standard of FG-2216. This product is intended for research and analytical applications. FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.
    FG-2216 (Standard)
  • HY-N15497
    Terpestacin
    		Inhibitor
    Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity.
    Terpestacin
  • HY-N0493R
    Pectolinarigenin (Standard)
    		Inhibitor
    Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
    Pectolinarigenin (Standard)
  • HY-101028R
    ZINC13466751 (Standard)
    		Inhibitor
    ZINC13466751 (Standard) is the analytical standard of ZINC13466751 (HY-101028). This product is intended for research and analytical applications. ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.
    ZINC13466751 (Standard)
  • HY-N0433R
    Astragaloside II (Standard)
    		Inhibitor
    Astragaloside II (Standard) is the analytical standard of Astragaloside II (HY-N0433). This product is intended for research and analytical applications. Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis.
    Astragaloside II (Standard)
  • 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-100543R
    Zenidolol (Standard)
    		Inhibitor
    Zenidolol (ICI-118551) (Standard) is the analytical standard of Zenidolol (HY-100543). This product is intended for research and analytical applications. Zenidolol is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.
    Zenidolol (Standard)
  • HY-100575R
    Acriflavine (Standard)
    		Inhibitor
    Acriflavine (Standard) is the analytical standard of Acriflavine (HY-100575). This product is intended for research and analytical applications. Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2.
    Acriflavine (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>
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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