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-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-13426S
    Roxadustat-d5
    		Inhibitor 98.80%
    Roxadustat-d5 is deuterium labeled Roxadustat. Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.
    Roxadustat-d<sub>5</sub>
  • HY-100947A
    cis VH-298
    		Inhibitor
    cis VH-298 is the cis form of VH-298 (HY-100947). cis VH-298 results in a significant loss of binding specificity of hydroxylated HIF-1a peptides to VHL in vitro.
    cis VH-298
  • HY-118543
    TM6089
    		Activator 99.37%
    TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector.
    TM6089
  • 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-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-16031B
    AFP464 dihydrochloride
    		Inhibitor 99.67%
    AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).
    AFP464 dihydrochloride
  • HY-18370
    HIF-2α-IN-3
    		Inhibitor 99.89%
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
    HIF-2α-IN-3
  • 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-B0413R
    Fenbendazole (Standard)
    		Activator
    Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53.
    Fenbendazole (Standard)
  • HY-114333
    Octyl-α-ketoglutarate
    		Activator
    Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD.
    Octyl-α-ketoglutarate
  • 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-W654013
    Minocycline-d7
    		Inhibitor
    Minocycline-d7 is deuterium labeled Minocycline. 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-d<sub>7</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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