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-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-159644
    Casdatifan
    		Inhibitor
    Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC.
    Casdatifan
  • HY-119264
    PRLX-93936
    		Inhibitor 98.31%
    PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma.
    PRLX-93936
  • 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-108868
    Mersalyl
    		Inducer
    Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.
    Mersalyl
  • 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-147029
    HIF1 agonist-1
    		Agonist 99.11%
    HIF1 agonist-1 (compound F4) is a potent HIF1 agonist with an EC50 value of 0.9 μM. HIF1 agonist-1 can be used for researching anticancer.
    HIF1 agonist-1
  • 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-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-112068
    DM-NOFD
    		Inhibitor 99.81%
    DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF).
    DM-NOFD
  • HY-112374
    NPAS3-IN-1
    		Inhibitor 98.72%
    NPAS3-IN-1 is a potent inhibitor of NPAS3-ARNT heterodimerization and regulates NPAS3 transcription by disrupting the heterodimerization of NPAS3 with ARNT at the cellular level.
    NPAS3-IN-1
  • HY-116893
    Diethyl bipy55'DC
    		Inhibitor 98.79%
    Diethyl bipy55'DC is an inhibitor of collagen proline 4-hydroxylases (CP4Hs) with antifibrotic and anti-metastatic activities. Diethyl bipy55'DC can inhibit CP4H activity in cultured cells at concentrations that do not cause iron deficiency.
    Diethyl bipy55'DC
  • 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-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-N7064
    Iminostilbene
    		Inhibitor 99.34%
    Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
    Iminostilbene
  • 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-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
  • HY-128578
    KPLH1130
    		Inhibitor 99.86%
    KPLH1130 is a pyruvate dehydrogenase kinase (PDK) inhibitor. KPLH1130 potently inhibits M1 macrophage polarization by reducing the expression of pro-inflammatory cytokines, decreasing the levels of M1 phenotype markers (HIF-1α, iNOS) and nitric oxide (NO) production. KPLH1130 prevents the reduction of mitochondrial oxygen consumption rate (OCR) induced by inflammatory stimuli (LPS ((HY-D1056) + IFN-γ) in various macrophage types. KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 can be used for the study of obesity-associated metabolic disorders and other inflammatory conditions.
    KPLH1130
  • HY-101028
    ZINC13466751
    		Inhibitor 99.94%
    ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.
    ZINC13466751
  • HY-44809
    Izilendustat
    		Inhibitor 98.01%
    Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.
    Izilendustat
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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