1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase

HIF/HIF Prolyl-Hydroxylase

Hypoxia-inducible factors; HIFs; HIF-PH

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-117479
    CL67
    Inhibitor
    CL67 is a potent hypoxia-inducible factor (HIF) pathway inhibitor. CL67 interferes G-quadruplex structures within promoter sequences. CL67 can be used in research of renal cancer.
    CL67
  • HY-149491
    HIV-IN-7
    Inhibitor
    Axl-IN-16 (Compound 4) is a Axl inhibitor. Axl-IN-16 inhibits Axl expression and inhibits the activity of HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 can be isolated from“fruiting liquid (FL)” of Hypholoma lateritium and Hericium erinaceus.
    HIV-IN-7
  • HY-156526
    PHD-IN-1
    Inhibitor
    PHD-IN-1 (compound 80) is a potent inhibitor of PHD2,with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells,respectively.
    PHD-IN-1
  • HY-N10330
    7-Hydroxyneolamellarin A
    Inhibitor
    7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer.
    7-Hydroxyneolamellarin A
  • HY-163602
    HIF-2α-IN-15
    Inhibitor
    HIF-2α-IN-15 (35) is a HIF-2α inhibitor, with an IC50 of 0.41 μM.
    HIF-2α-IN-15
  • HY-161660
    DS44470011
    Inhibitor
    DS44470011 is a hypoxia-inducing factor prolyl hydroxylase (HIF-PHD) inhibitor. DS44470011 has oral activity. DS44470011 promotes cell release of erythropoietin (EPO). DS44470011 can be used in the research of renal anemia.
    DS44470011
  • HY-141625
    TRC160334
    Inhibitor
    TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 can be used for the research of ischemia/reperfusion injury.
    TRC160334
  • HY-P10797
    TAT-N24
    Inhibitor
    TAT-N24 is a cell-permeable TAT peptide as a p55PIK signaling inhibitor. TAT-N24 is effective for corneal neovascularization (CNV) and ocular inflammation by inhibiting the HIF-1α/NF-κB signaling pathway in corneal suture (CS). TAT-N24 also inhibits corneal neovascularization.
    TAT-N24
  • HY-14575
    Nastorazepide hemicalcium
    Inhibitor
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide hemicalcium
  • HY-P991664
    AG01
    Inhibitor
    AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers.
    AG01
  • HY-163839
    DS-1093a
    Inhibitor
    DS-1093a is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitor, with an EC50 of 0.49 μM in Hep3B cell EPO production. DS-1093a can be used in the research of renal anemia.
    DS-1093a
  • HY-77554R
    Cephalomannine (Standard)
    Cephalomannine (Standard) is the analytical standard of Cephalomannine. This product is intended for research and analytical applications. Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog that can be isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
    Cephalomannine (Standard)
  • 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
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