1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase

HIF/HIF Prolyl-Hydroxylase

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 Related Products (47):

Cat. No. Product Name Effect Purity
  • HY-12867
    PT-2385 Inhibitor 99.48%
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
  • HY-15893
    DMOG Inhibitor 99.15%
    DMOG (Dimethyloxallyl Glycine) is a cell-permeable and competitive inhibitor of HIF-1α prolyl hydroxylase (HIF-PH).
  • HY-13426
    Roxadustat Inhibitor 99.91%
    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.
  • HY-10231
    PX-478 Inhibitor >98.0%
    PX-478 is an antitumor inhibitor of hypoxia-inducible factor-1α (HIF-1α).
  • HY-15836
    BAY 87-2243 Inhibitor 99.41%
    BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
  • HY-108697
    PT2399 Antagonist 99.88%
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
  • HY-125840
    PT2977 Inhibitor
    PT2977 is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC).
  • HY-128872
    VCE-​004.8 Activator
    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity. VCE-004.8 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. VCE-004.8 attenuates adipogenesis and prevents diet-induced obesity.
  • HY-101277
    Vadadustat Inhibitor 99.63%
    Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
  • HY-13671
    LW6 Inhibitor >98.0%
    LW6 is a novel HIF-1 inhibitor with an IC50 of 4.4 μM.
  • HY-12519
    Oltipraz Inhibitor 99.82%
    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.
  • HY-17608
    Daprodustat Inhibitor 99.39%
    Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
  • HY-N0055
    Chlorogenic acid Inhibitor 99.29%
    Chlorogenic acid is a major phenolic compound in coffee and tea. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension.
  • HY-18777
    KC7F2 Inhibitor 99.61%
    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.
  • HY-12654
    Molidustat Inhibitor 98.33%
    Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
  • HY-N0560
    Oroxylin A Inhibitor 99.90%
    Oroxylin A is a natural active flavonoid with strong anticancer effects.
  • HY-N0892
    AKBA Inhibitor 99.71%
    AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
  • HY-100575
    Acriflavine Inhibitor 98.62%
    Acriflavine is a fluorescent dye for labeling high molecular weight RNA. It is also a topical antiseptic.
  • HY-103227
    Desidustat Inhibitor 99.49%
    Desidustat is an inhibitor of HIF hydroxylase extracted from patent WO 2014102818 A1, compound example 2.
  • HY-B0464
    Hydralazine hydrochloride Activator >98.0%
    Hydralazine hydrochloride is a direct-acting vasodilator that is used as an antihypertensive agent.
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