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-N3244
    Moracin O
    		Inhibitor 99.98%
    Moracin O is a 2-arylbenzofuran isolated from the Morus alba Linn. . Moracin O exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects.
    Moracin O
  • HY-119264A
    PRLX-93936 dihydrochloride
    		Inhibitor 99.83%
    PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma.
    PRLX-93936 dihydrochloride
  • HY-110036A
    GW405833 hydrochloride
    		Inhibitor 99.59%
    GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).
    GW405833 hydrochloride
  • HY-153017
    HIF-1 inhibitor-4
    		Inhibitor 99.50%
    HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
    HIF-1 inhibitor-4
  • HY-N1437
    Hydroxycitric acid
    		Inhibitor 98.79%
    Hydroxycitric acid is the major active ingredient of Garcinia cambogia. Hydroxycitric acid competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
    Hydroxycitric acid
  • HY-128872
    Etrinabdione
    		Activator 99.16%
    Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity.
    Etrinabdione
  • HY-136748
    HIF-2α-IN-4
    		Inhibitor 99.96%
    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-123422
    GSK360A
    		Inhibitor 99.90%
    GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
    GSK360A
  • HY-19621
    THS-044
    		Modulator 99.67%
    THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings.
    THS-044
  • HY-151344
    HIF-1/2α-IN-2
    		Inhibitor 99.55%
    HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).
    HIF-1/2α-IN-2
  • HY-122094
    Steppogenin
    		Inhibitor 99.49%
    Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
    Steppogenin
  • HY-N5112
    (Rac)-Arnebin 1
    		99.88%
    (Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity.
    (Rac)-Arnebin 1
  • HY-N3243
    Moracin P
    		Inhibitor 99.57%
    Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects.
    Moracin P
  • HY-168641
    PROTAC HIF-1α degrader-1
    		Degrader 98.02%
    PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis. (Pink: ligand for target protein (HY-111387); black: linker (HY-W013731); Blue: E3 ligase ligand (HY-112078)).
    PROTAC HIF-1α degrader-1
  • HY-P1888
    HIF-1 alpha (556-574)
    		99.37%
    HIF-1 alpha (556-574) is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis.
    HIF-1 alpha (556-574)
  • HY-17617
    Nastorazepide
    		Inhibitor 99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide
  • HY-136300
    PHD-1-IN-1
    		Inhibitor 99.21%
    PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an "Arg367-out" pocket.
    PHD-1-IN-1
  • HY-N0055R
    Chlorogenic acid (Standard)
    		Inhibitor
    Chlorogenic acid (Standard) is the analytical standard of Chlorogenic acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B2141
    Bendazol
    		Inhibitor 99.78%
    Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats.
    Bendazol
  • HY-N0733S3
    Glucosamine-6-13C hydrochloride
    		≥98.0%
    Glucosamine-6-13C (hydrochloride) is the 13C labeled Glucosamine hydrochloride. 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
    Glucosamine-6-<sup>13</sup>C hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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