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-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-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>
  • HY-147813
    HIF-1α-IN-3
    		Inhibitor
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency.
    HIF-1α-IN-3
  • HY-163601
    HIF-2α-IN-14
    		Inhibitor
    HIF-2α-IN-14 (18) is a HIF-2α inhibitor, with an IC50 of 0.27 μM.
    HIF-2α-IN-14
  • HY-N0234R
    Bavachinin (Standard)
    		Inhibitor
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..
    Bavachinin (Standard)
  • HY-172257
    HIF-PHD-IN-4
    		Inhibitor
    HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. HIF-PHD-IN-4 can effectively enhance the mobilization of hematopoietic stem cells induced by G-CSF in mice at a dose of 2 mg/kg. HIF-PHD-IN-4 is suitable for research in the field of tumor therapy .
    HIF-PHD-IN-4
  • HY-170915
    DDO-3055
    		Inhibitor
    DDO-3055 is an orally active PHD2 inhibitor that can be used in the research of anemia associated with chronic kidney disease.
    DDO-3055
  • HY-163598
    HIF-2α-IN-11
    		Inhibitor
    HIF-2α-IN-11 (1) is a HIF-2α inhibitor, with an IC50 of 59.2 nM.
    HIF-2α-IN-11
  • HY-177078
    Davotifan
    		Inhibitor
    Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer.
    Davotifan
  • HY-144332
    PHD2/HDACs-IN-1
    		Inhibitor
    PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI).
    PHD2/HDACs-IN-1
  • HY-12519S
    Oltipraz-d3
    		Inhibitor
    Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz-d<sub>3</sub>
  • HY-161427
    HSP90-IN-30
    		Inhibitor
    HSP90-IN-30 (compound 3e) inhibits HSP90 chaperone activity. HSP90-IN-30 inhibits the activity of HIF-1 transcriptional under hypoxia with an IC50 value of 2.16 μM.
    HSP90-IN-30
  • HY-15468A
    IOX2 sodium
    		Inhibitor
    IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases.
    IOX2 sodium
  • HY-12519G
    Oltipraz (GMP)
    		Activator
    Oltipraz (GMP) is Oltipraz (HY-12519) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Oltipraz has an inhibitory effect on HIF-1α activation. Oltipraz is a potent Nrf2 activator.
    Oltipraz (GMP)
  • HY-N1098R
    Velutin (Standard)
    		Inhibitor
    Colchiceine (Standard) is the analytical standard of Colchiceine. This product is intended for research and analytical applications. Colchiceine is one of several metabolites of the anti-gout medication Colchicine (HY-16569). Colchicine is a tubulin inhibitor and a microtubule disrupting agent, and may protect rats from developing liver injury and fibrosis.
    Velutin (Standard)
  • HY-P1420A
    TAT-cyclo-CLLFVY TFA
    		Inhibitor
    TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
    TAT-cyclo-CLLFVY TFA
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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