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-W613220
    MDH1/2-IN-1
    		Inhibitor 99.53%
    MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 nM and 1.06 nM respectively). MDH1/2-IN-1 inhibits mitochondrial respiration and the HIF-1α pathway. MDH1/2-IN-1 demonstrates significant anti-tumor potential. MDH1/2-IN-1 provides a new direction for the development of drugs targeting cancer metabolism.
    MDH1/2-IN-1
  • HY-147029
    HIF1 agonist-1
    		Agonist 99.11%
    HIF1 agonist-1 (compound F4) is a potent HIF1 agonist with an EC50 value of 0.9 μM. HIF1 agonist-1 can be used for researching anticancer.
    HIF1 agonist-1
  • HY-N0733S3
    Glucosamine-6-13C hydrochloride
    		98.0%
    Glucosamine-6-13C (hydrochloride) is the 13C 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, is used as
    Glucosamine-6-<sup>13</sup>C hydrochloride
  • 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-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-148860
    NVP-DFF332
    		Inhibitor 99.31%
    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-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
  • HY-16196
    ENMD-1198
    		Inhibitor 98.87%
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
    ENMD-1198
  • HY-159120
    ZG-2291
    		Inhibitor 98.08%
    ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases.
    ZG-2291
  • 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-B2141
    Bendazol
    		Inhibitor 99.78%
    Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats.
    Bendazol
  • 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-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-P10426
    cyclo(CLLFVY)
    		Inhibitor 99.37%
    cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers.
    cyclo(CLLFVY)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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