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-B0988
    Deferoxamine mesylate
    		Activator 99.86%
    Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
    Deferoxamine mesylate
  • HY-15893
    DMOG
    		Inhibitor 99.69%
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
    DMOG
  • HY-10231
    PX-478
    		Inhibitor ≥98.0%
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
    PX-478
  • HY-17412
    Minocycline hydrochloride
    		Inhibitor 99.79%
    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 hydrochloride
  • HY-13426
    Roxadustat
    		Inhibitor 99.91%
    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
  • HY-158341
    IOX5
    		Inhibitor 99.39%
    IOX5 is a selective prolyl hydroxylases (PHD) inhibitor. IOX5 stabilizes HIF-1α in AML cells, induces apoptosis, and upregulates BNIP3 expression. IOX5 compromises development and progression of acute myeloid leukemia.
    IOX5
  • HY-W009156R
    Citric acid tripotassium hydrate (Standard)
    		Inhibitor
    Citric acid (tripotassium hydrate) (Standard) is the analytical standard of Citric acid (tripotassium hydrate). This product is intended for research and analytical applications. Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
    Citric acid tripotassium hydrate (Standard)
  • HY-159644
    Casdatifan
    		Inhibitor
    Casdatifan
  • HY-125840
    Belzutifan
    		Inhibitor 99.85%
    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
  • HY-13671
    LW6
    		Inhibitor 98.38%
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
    LW6
  • HY-B0239
    Chloramphenicol
    		Inhibitor 99.82%
    Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
    Chloramphenicol
  • HY-N0055
    Chlorogenic acid
    		Inhibitor 99.55%
    Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb. It is an orally active antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension compound.
    Chlorogenic acid
  • HY-12867
    PT-2385
    		Inhibitor 99.95%
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
    PT-2385
  • HY-17608
    Daprodustat
    		Inhibitor 99.80%
    Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
    Daprodustat
  • HY-B1625
    Deferoxamine
    		Activator 99.76%
    Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
    Deferoxamine
  • HY-15836
    BAY 87-2243
    		Inhibitor 99.41%
    BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
    BAY 87-2243
  • HY-B0639
    Amifostine
    		Activator ≥98.0%
    Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action.
    Amifostine
  • HY-12654
    Molidustat
    		Inhibitor 98.75%
    Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia.
    Molidustat
  • HY-B1125
    Glucosamine
    		Inhibitor ≥98.0%
    Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine 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
  • HY-18777
    KC7F2
    		Inhibitor 99.64%
    KC7F2 is a potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor with an IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent.
    KC7F2
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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