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-15641
    FG-2216
    		Inhibitor 99.49%
    FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.
    FG-2216
  • HY-W009156
    Citric acid tripotassium hydrate
    		Inhibitor ≥99.0%
    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
  • HY-N0242
    Fraxinellone
    		Inhibitor 99.99%
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
    Fraxinellone
  • HY-111387
    IDF-11774
    		Inhibitor 99.87%
    IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
    IDF-11774
  • HY-12832
    JNJ-42041935
    		Inhibitor 99.79%
    JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.
    JNJ-42041935
  • HY-N0910
    Notoginsenoside Ft1
    		≥98.0%
    Notoginsenoside Ft1 is a saponin isolated from Panax notoginseng; stimulator of angiogenesis.
    Notoginsenoside Ft1
  • HY-110266
    GN44028
    		Inhibitor 99.48%
    GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.
    GN44028
  • HY-18371
    TC-S 7009
    		Inhibitor 99.64%
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
    TC-S 7009
  • HY-111547
    M1001
    		Agonist 99.86%
    M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.
    M1001
  • HY-113649
    AKB-6899
    		Inhibitor 99.95%
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
    AKB-6899
  • HY-115903
    HIF-1α-IN-2
    		Inhibitor 98.45%
    HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
    HIF-1α-IN-2
  • HY-W088075
    Acriflavine hydrochloride
    		Inhibitor
    Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic. Acriflavine hydrochloride is a potent HIF-1 inhibitor, with antitumor activity. Acriflavine hydrochloride has antimicrobial and antiviral activities. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2
    Acriflavine hydrochloride
  • HY-B0413S
    Fenbendazole-d3
    		Activator 99.46%
    Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
    Fenbendazole-d<sub>3</sub>
  • HY-N5112A
    β,β-Dimethylacrylalkannin
    		99.36%
    β,β-Dimethylacrylalkannin (Arnebin 1) is a napthoquinone isolated from Alkanna cappadocica , increases collagen and involucrin content in skin cells.
    β,β-Dimethylacrylalkannin
  • HY-137239
    1,4-DPCA ethyl ester
    		Inhibitor 99.52%
    1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
    1,4-DPCA ethyl ester
  • HY-77554
    Cephalomannine
    		98.49%
    Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog that can be isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
    Cephalomannine
  • HY-100693
    SYP-5
    		Inhibitor 98.64%
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
    SYP-5
  • HY-P1420
    TAT-cyclo-CLLFVY
    		Inhibitor 98.06%
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
    TAT-cyclo-CLLFVY
  • HY-136748
    HIF-2α-IN-4
    		Inhibitor 99.91%
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
    HIF-2α-IN-4
  • HY-W016409
    Ethyl 3,4-dihydroxybenzoate
    		Inhibitor 99.87%
    Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect.
    Ethyl 3,4-dihydroxybenzoate
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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