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-139804
    CTK7A
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer treatment research.
    CTK7A
  • HY-119264
    PRLX-93936
    		Inhibitor
    PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma.
    PRLX-93936
  • HY-158826
    EZN-2968
    EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.
    EZN-2968
  • HY-N14340
    Fibrostatin F
    		Inhibitor
    Fibrostatin F is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin F
  • HY-29090
    ML228 analog
    		Activator
    ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF.
    ML228 analog
  • HY-N0487R
    Glucosamine sulfate (Standard)
    		Inhibitor
    Glucosamine (sulfate) (Standard) is the analytical standard of Glucosamine (sulfate). This product is intended for research and analytical applications. Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate 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 sulfate (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-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
  • HY-139855
    ZG-2033
    		Agonist
    ZG-2033 (Compound 26) is an orally active HIF-2α agonist that demonstrates nanomolar activity in luciferase reporter gene assays (EC50 = 490 nM). ZG-2033 has the effect of alleviating anemia and exhibits synergistic action with AKB-6548 (HY-101277) in anemia, and can be used in the study of renal anemia.
    ZG-2033
  • HY-101277S1
    Vadadustat-13C6
    		Inhibitor
    Vadadustat-13C6 (PG-1016548-13C6) is 13C labeled Vadadustat. Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
    Vadadustat-<sup>13</sup>C<sub>6</sub>
  • HY-125840R
    Belzutifan (Standard)
    		Inhibitor
    Belzutifan (Standard) is the analytical standard of Belzutifan. This product is intended for research and analytical applications. Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
    Belzutifan (Standard)
  • HY-13426R
    Roxadustat (Standard)
    		Inhibitor
    Roxadustat (Standard) is the analytical standard of Roxadustat. This product is intended for research and analytical applications. Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.
    Roxadustat (Standard)
  • HY-N14330
    Fibrostatin A
    		Inhibitor
    Fibrostatin A is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin A
  • HY-158826A
    EZN-2968 sodium
    EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.
    EZN-2968 sodium
  • HY-N14339
    Fibrostatin E
    		Inhibitor
    Fibrostatin E is a proline hydroxylase inhibitor found in Strptomyces catenulae.
    Fibrostatin E
  • HY-15641R
    FG-2216 (Standard)
    		Inhibitor
    FG-2216 (Standard) is the analytical standard of FG-2216. This product is intended for research and analytical applications. FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.
    FG-2216 (Standard)
  • HY-112068
    DM-NOFD
    		Inhibitor
    DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF).
    DM-NOFD
  • HY-N15497
    Terpestacin
    		Inhibitor
    Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity.
    Terpestacin
  • HY-N0433R
    Astragaloside II (Standard)
    		Inhibitor
    Astragaloside II (Standard) is the analytical standard of Astragaloside II (HY-N0433). This product is intended for research and analytical applications. Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis.
    Astragaloside II (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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