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-N0892R
    AKBA (Standard)
    		Inhibitor
    AKBA (Standard) is the analytical standard of AKBA. This product is intended for research and analytical applications. AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
    AKBA (Standard)
  • HY-16031
    AFP464 free base
    		Inhibitor
    AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
    AFP464 free base
  • HY-151465
    HIF-1α-IN-4
    		Inhibitor 99.95%
    HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer.
    HIF-1α-IN-4
  • HY-148230
    TFEB Decoy ODN sodium
    		Inhibitor
    TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
    TFEB Decoy ODN sodium
  • HY-161313
    DYB-03
    		Inhibitor 99.49%
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2- and GSK126-resistant of A549 and H460 cells.
    DYB-03
  • HY-N0416R
    Cucurbitacin B (Standard)
    Cucurbitacin B (Standard) is the analytical standard of Cucurbitacin B. This product is intended for research and analytical applications. Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.
    Cucurbitacin B (Standard)
  • HY-P10221A
    Cyclo(CKLIIF) TFA
    		Inhibitor
    Cyclo CKLIIF 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 2.6 and 2.2 μM, respectively.
    Cyclo(CKLIIF) TFA
  • HY-B0464S
    Hydralazine-d4 hydrochloride
    		Activator
    Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is a direct-acting vasodilator that is used as an antihypertensive agent.
    Hydralazine-d<sub>4</sub> hydrochloride
  • HY-112678
    TM6008
    		Inhibitor 99.51%
    TM6008 is a potent and orally active prolyl hydroxylase (PHD) inhibitor. TM6008 chelats transition metal (copper) and inhibits the autoxidation of ascorbic acid with an IC50 value is 0.57 μM. TM6008  exerts organ protection against ischemia in vivo and can be used for cerebrovascular disease research.
    TM6008
  • HY-B0223R
    Albendazole (Standard)
    		Inhibitor
    Albendazole (Standard) is the analytical standard of Albendazole. This product is intended for research and analytical applications. Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells.
    Albendazole (Standard)
  • 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-17412A
    Minocycline
    		Inhibitor
    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
  • HY-136055
    (S,R,S)-AHPC-C5-COOH
    		Inhibitor 98.81%
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
    (S,R,S)-AHPC-C5-COOH
  • HY-151341
    HIF-1/2α-IN-1
    		Inhibitor
    HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
    HIF-1/2α-IN-1
  • HY-148264
    Imdatifan
    		Inhibitor
    Imdatifan (HIF-2α-IN-7) is a hypoxia inducible factor 2α (HIF-2α) inhibitor. Imdatifan can inhibit HIF-2α with an EC50 value of 6 nM. Imdatifan can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders.
    Imdatifan
  • HY-159644
    Casdatifan
    		Inhibitor
    Casdatifan
  • HY-109057A
    Enarodustat hydrochloride
    		Inhibitor
    Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.
    Enarodustat hydrochloride
  • HY-44809A
    Izilendustat hydrochloride
    		Inhibitor
    Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
    Izilendustat hydrochloride
  • HY-144178
    HIF-2α-IN-6
    		Inhibitor
    HIF-2α-IN-6 (117) is a HIF-2α inhibitor.
    HIF-2α-IN-6
  • HY-112441
    Prolyl Hydroxylase inhibitor 1
    		Inhibitor
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
    Prolyl Hydroxylase inhibitor 1
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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