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-108697A
    (Rac)-PT2399
    		Inhibitor 99.84%
    (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
  • HY-44809
    Izilendustat
    		Inhibitor 99.20%
    Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
    Izilendustat
  • HY-N1098
    Velutin
    		Inhibitor 98.60%
    Velutin is an aglycone extracted from Flammulina velutipes, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway.
    Velutin
  • HY-142693
    Angiogenesis agent 1
    		Activator 99.39%
    Angiogenesis agent 1 (compound C-31) is a salidroside-derivated glycoside analogue. Angiogenesis agent 1 is an activator of the HIF-1α pathway. Angiogenesis agent 1 has the potential for the research of diabetic hind limb ischemia.
    Angiogenesis agent 1
  • HY-147029
    HIF1-IN-3
    		Inhibitor 99.11%
    HIF1-IN-3 (compound F4) is a potent HIF1 inhibitor with an EC50 value of 0.9 μM. HIF1-IN-3 can be used for researching anticancer.
    HIF1-IN-3
  • HY-101028
    ZINC13466751
    		Inhibitor 99.94%
    ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.
    ZINC13466751
  • HY-116893
    Diethyl bipy55'DC
    		Inhibitor 98.79%
    Diethyl bipy55'DC is an inhibitor of collagen proline 4-hydroxylases (CP4Hs) with antifibrotic and anti-metastatic activities. Diethyl bipy55'DC can inhibit CP4H activity in cultured cells at concentrations that do not cause iron deficiency.
    Diethyl bipy55'DC
  • HY-148860
    NVP-DFF332
    		Inhibitor 99.85%
    HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity.
    NVP-DFF332
  • HY-112374
    NPAS3-IN-1
    		Inhibitor 98.29%
    NPAS3-IN-1 is a potent inhibitor of NPAS3-ARNT heterodimerization and regulates NPAS3 transcription by disrupting the heterodimerization of NPAS3 with ARNT at the cellular level.
    NPAS3-IN-1
  • HY-N0733R
    Glucosamine hydrochloride (Standard)
    		Inhibitor
    Glucosamine (hydrochloride) (Standard) is the analytical standard of Glucosamine (hydrochloride). This product is intended for research and analytical applications. 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 dietary supplement. Glucosamine hydrochloride 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 hydrochloride (Standard)
  • HY-19949
    HIF-2α-IN-1
    		Inhibitor 99.94%
    HIF-2α-IN-1 (compound 9b) is a HIF-2α inhibitor (IC50=1.7 μM, SPA/scintillation proximity assay).
    HIF-2α-IN-1
  • HY-16187
    EL-102
    		Inhibitor 99.44%
    EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
    EL-102
  • HY-131346
    HIF-PHD-IN-1
    		Inhibitor 99.37%
    HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia.
    HIF-PHD-IN-1
  • HY-151466
    HIF-1α-IN-5
    		Inhibitor 99.95%
    HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer.
    HIF-1α-IN-5
  • HY-119351
    BNS
    		Inhibitor
    BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.
    BNS
  • HY-100947A
    cis VH-298
    		Inhibitor 99.96%
    cis VH-298 is the cis form of VH-298 (HY-100947). cis VH-298 results in a significant loss of binding specificity of hydroxylated HIF-1a peptides to VHL in vitro.
    cis VH-298
  • HY-148230
    TFEB Decoy ODN sodium
    		Inhibitor
    TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
    TFEB Decoy ODN sodium
  • HY-168533
    ZG-2305
    		Inhibitor
    ZG-2305 is a potent, orally active and selective factor inhibiting hypoxia-inducible factor (FIH) inhibitor with Ki values of 79.6, 2786 nM for FIH, PHD2, respectively. ZG-2305 increases the expression of EGLN3 gene. ZG-2305 decreases the cellular triglycerides levels and reduces lipid accumulation. ZG-2305 has the potential for the research of obesity and fatty liver disease.
    ZG-2305
  • HY-161313
    DYB-03
    		Inhibitor 99.49%
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2- and GSK126-resistant of A549 and H460 cells.
    DYB-03
  • HY-N7064
    Iminostilbene
    		Inhibitor 99.34%
    Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
    Iminostilbene
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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