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. 상품명 효과 Purity Chemical Structure
  • HY-179439
    Multi-kinase-IN-8
    		Inhibitor
    Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
    Multi-kinase-IN-8
  • HY-146540
    GEM-5
    		Inhibitor
    GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
    GEM-5
  • HY-17412AS
    Minocycline-d6
    		Inhibitor
    Minocycline-d6 is deuterium labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
    Minocycline-d<sub>6</sub>
  • HY-163603
    HIF-2α-IN-16
    		Inhibitor
    HIF-2α-IN-16 (48) is a HIF-2α inhibitor, with an IC50 of 0.091 μM.
    HIF-2α-IN-16
  • HY-144176
    HIF-2α-IN-5
    		Inhibitor
    HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.
    HIF-2α-IN-5
  • HY-132974
    Aminoflavone
    		Inhibitor
    Aminoflavone is an anti-tumor agent. Aminoflavone inhibits the expression of ITGA6/SOX2 by activating the AhR-miR-125b-2-3p axis, thereby targeting breast cancer stem cells. Aminoflavone induces an increase in intracellular ROS, increases the level of oxidative DNA damage marker 8-oxodG and DNA-protein cross-links. Aminoflavone causes S-phase arrest, activates caspase-3/8/9 and induces apoptosis (apoptosis). Aminoflavone inhibits HIF-1α expression in a manner independent of AhR. Aminoflavone can be used for the study of breast cancer.
    Aminoflavone
  • HY-156527
    PHD-IN-2
    		Inhibitor
    PHD-IN-2 (Compound 91) is a PHD antagonist (IC50: < 5 nM). PHD-IN-2 induces erythropoietin synthesis in HEP3B cells (EC50: <2.5 μM). PHD-IN-2 can be used for research of cardiovascular disorders, metabolic disorders, hematological disorders, pulmonary disorders, kidney disorders, liver disorders, wound healing disorders, and cancer.
    PHD-IN-2
  • HY-163370
    HIF-1α-IN-7
    		Inhibitor
    HIF-1α-IN-7 (Compound D13) is a potent HIF-1α inhibitor. HIF-1α-IN-7 has neuroprotective activity. HIF-1α-IN-7 can be used in Alzheimer's disease research.
    HIF-1α-IN-7
  • HY-162438
    PHD2-IN-2
    		Inhibitor
    PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia.
    PHD2-IN-2
  • HY-149886
    HIF-2α-IN-9
    		Inhibitor
    HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity.
    HIF-2α-IN-9
  • HY-176408
    PHD2-IN-5
    		Inhibitor
    PHD2-IN-5 (compound 22) is a potent PHD2 inhibitor with an IC50 of 0.82 μM. PHD2-IN-5 can be used in the study of renal anemia.
    PHD2-IN-5
  • HY-100947R
    VH-298 (Standard)
    		Inhibitor
    VH-298 (Standard) is the analytical standard of VH-298 (HY-100947). This product is intended for research and analytical applications. VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs.
    VH-298 (Standard)
  • HY-113662
    CLB-016
    		Inhibitor
    CLB-016 is a potent Hypoxia-inducible factor (HIF-1) inhibitor with an IC50 of 19.1 μM. CLB-016 significantly suppresses HIF-1-mediated hypoxia response.
    CLB-016
  • HY-N14340
    Fibrostatin F
    		Inhibitor
    Fibrostatin F is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin F
  • HY-101023R
    MK-8617 (Standard)
    		Inhibitor
    MK-8617 (Standard) is the analytical standard of MK-8617 (HY-101023). This product is intended for research and analytical applications. MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
    MK-8617 (Standard)
  • HY-10231R
    PX-478 (Standard)
    		Inhibitor
    PX-478 (Standard) is the analytical standard of PX-478 (HY-10231). This product is intended for research and analytical applications. PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
    PX-478 (Standard)
  • HY-N2518R
    Agnuside (Standard)
    		Inhibitor
    Agnuside (Standard) is the analytical standard of Agnuside. This product is intended for research and analytical applications. Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.
    Agnuside (Standard)
  • HY-N14332
    Fibrostatin D
    		Inhibitor
    Fibrostatin D is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin D
  • HY-101449R
    Adaptaquin (Standard)
    		Inhibitor
    Adaptaquin (Standard) is the analytical standard of Adaptaquin (HY-101449). This product is intended for research and analytical applications. Adaptaquin is a BBB-penetrable HIF-PHDs inhibitor. Adaptaquin has anti-inflammatory and neuroprotective effects. Adaptaquin can effectively inhibit lipid peroxidation, maintain mitochondrial function, and reduce neuronal death. Adaptaquin can be used in the research of nervous system diseases such as Parkinson's disease.
    Adaptaquin (Standard)
  • HY-123009
    KCN1
    		Inhibitor
    KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest.
    KCN1
Cat. No. 상품명 / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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