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-109057A
    Enarodustat hydrochloride
    		Inhibitor
    Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.
    Enarodustat hydrochloride
  • HY-44809A
    Izilendustat hydrochloride
    		Inhibitor
    Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
    Izilendustat hydrochloride
  • HY-144178
    HIF-2α-IN-6
    		Inhibitor
    HIF-2α-IN-6 (117) is a HIF-2α inhibitor.
    HIF-2α-IN-6
  • HY-112441
    Prolyl Hydroxylase inhibitor 1
    		Inhibitor
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
    Prolyl Hydroxylase inhibitor 1
  • HY-N0560R
    Oroxylin A (Standard)
    		Inhibitor
    Oroxylin A (Standard) is the analytical standard of Oroxylin A. This product is intended for research and analytical applications. Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis.
    Oroxylin A (Standard)
  • HY-169100
    Antiproliferative agent-57
    		Inhibitor
    Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.
    Antiproliferative agent-57
  • HY-141510A
    myo-Inositol trispyrophosphate hexa-triethylamine
    		≥98.0%
    myo-Inositol trispyrophosphate (ITPP) hexa-triethylamine is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate hexa-triethylamine is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate hexa-triethylamine enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate hexa-triethylamine can be used in the study of cardiovascular disease and cancer.
    myo-Inositol trispyrophosphate hexa-triethylamine
  • HY-N0596R
    Panaxadiol (Standard)
    		Inhibitor
    Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
    Panaxadiol (Standard)
  • HY-161586
    Chloramphenicol/BSA
    		Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-161265
    HIF-2α agonist 3
    		Agonist
    HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with a EC50 value of 1.78 μM. HIF-2α agonist 3 can be used in the study of renal anemia.
    HIF-2α agonist 3
  • HY-P1888A
    HIF-1 alpha (556-574) TFA
    HIF-1 alpha (556-574) TFA is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis.
    HIF-1 alpha (556-574) TFA
  • HY-18259
    103D5R
    		Inhibitor
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM.
    103D5R
  • HY-170027
    LW1564
    		Inhibitor
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.
    LW1564
  • HY-N6939R
    Pseudolaric Acid B (Standard)
    		Inducer
    Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cell apoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2.
    Pseudolaric Acid B (Standard)
  • HY-170522
    ISM012-042
    		Inhibitor
    ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.
    ISM012-042
  • HY-P10222
    Cyclo(CRLLIF)
    		Inhibitor
    Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively.
    Cyclo(CRLLIF)
  • HY-118672
    HNHA
    		Inhibitor 99.76%
    HNHA is a potent HDAC inhibitor with an IC50 of 100 nM. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer.
    HNHA
  • HY-173488
    NF-κB/HIF-1α-IN-1
    		Inhibitor
    NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2.
    NF-κB/HIF-1α-IN-1
  • HY-17412S
    Minocycline-d6 hydrochloride
    		Inhibitor
    Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
    Minocycline-d<sub>6</sub> hydrochloride
  • HY-W753956
    Iminostilbene-d10
    Iminostilbene-d10 is the deuterium labeled Iminostilbene (HY-N7064). 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-d<sub>10</sub>
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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