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-155009
    PHD2-IN-1
    		Inhibitor
    PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research.
    PHD2-IN-1
  • HY-N0733S2
    Glucosamine-13C,15N hydrochloride
    Glucosamine-13C,15N (hydrochloride) is the 13C and 15N 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, i
    Glucosamine-<sup>13</sup>C,<sup>15</sup>N hydrochloride
  • HY-N0242R
    Fraxinellone (Standard)
    		Inhibitor
    Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
    Fraxinellone (Standard)
  • HY-157444
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG
    		Inhibitor
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) is a potent adjuvant obtained by optimization of the structure of EGCG. 5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) decreases the expression of HIF-1α and CBR1 at both the mRNA and protein levels.
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG
  • HY-177271
    PHD2-IN-6
    		Inhibitor
    PHD2-IN-6 (Example 89) is a HIF prolyl hydroxylase 2 (PHD2) inhibitor with an IC50 of 31.6  nM. PHD2-IN-6 stimulates encoding erythropoietin (EPO) production. PHD2-IN-6 can be used for inflammatory diseases like inflammatory bowel disease (IBD) and rheumatoid arthritis research.
    PHD2-IN-6
  • HY-B1125R
    Glucosamine (Standard)
    		Inhibitor
    Isomogroside V (Standard) is the analytical standard of Isomogroside V. This product is intended for research and analytical applications. Isomogroside V is a sweetener, which extracted from Siraitia grosvenorii (Swingle).
    Glucosamine (Standard)
  • HY-129502
    Fibrostatin C
    		Inhibitor
    Fibrostatin C (P-23924C) is an orally active prolyl hydroxylase inhibitor that also inhibits collagen biosynthesis. Fibrostatin C also increases the number of cytoplasmic granules immunoreactive with antibodies to collagen I or III. Fibrostatin C inhibits the secretion of type I collagen in Tenon's capsule fibroblasts. Fibrostatin C is promising for research of the wound fibrotic response in the wound of glaucoma filtering surgery.
    Fibrostatin C
  • HY-175521
    HIF-1α-IN-8
    		Inhibitor
    HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).
    HIF-1α-IN-8
  • HY-N0733S1
    Glucosamine-2-13C hydrochloride
    Glucosamine-2-13C (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
    Glucosamine-2-<sup>13</sup>C hydrochloride
  • HY-163148
    PHD-IN-3
    		Inhibitor
    PHD-IN-3 (Compound 15) is an orally active PHD inhibitor. PHD-IN-3 can be used in the study of anemia associated with chronic kidney disease.
    PHD-IN-3
  • HY-163512
    Anti-inflammatory agent 79
    		Inhibitor
    Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.
    Anti-inflammatory agent 79
  • HY-141625A
    TRC160334 sodium
    		Inhibitor
    TRC160334 sodium is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 sodium can be used for the research of ischemia/reperfusion injury.
    TRC160334 sodium
  • HY-163600
    HIF-2α-IN-13
    		Inhibitor
    HIF-2α-IN-13 (18) is a HIF-2α inhibitor, with an IC50 of 2.7 μM.
    HIF-2α-IN-13
  • HY-172201
    NF-κB-IN-19
    		Inhibitor
    NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
    NF-κB-IN-19
  • HY-124079
    HIF-1/2α-IN-3
    HIF-1/2α-IN-3 (compund 33) is a HIF-1/2α inhibitor.
    HIF-1/2α-IN-3
  • HY-W016409R
    Ethyl 3,4-dihydroxybenzoate (Standard)
    		Inhibitor
    Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema.
    Ethyl 3,4-dihydroxybenzoate (Standard)
  • HY-124722
    OHM1
    		Inhibitor
    OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM.
    OHM1
  • HY-N12041
    Axl-IN-16
    		Inhibitor
    Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression.
    Axl-IN-16
  • HY-163599
    HIF-2α-IN-12
    		Inhibitor
    HIF-2α-IN-12 (9) is a HIF-2α inhibitor, with an IC50 of 0.9 μM.
    HIF-2α-IN-12
  • HY-N0733S4
    Glucosamine-15N hydrochloride
    Glucosamine-15N (hydrochloride) is the 15N 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>15</sup>N hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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