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-16196
    ENMD-1198
    		Inhibitor 98.87%
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
    ENMD-1198
  • HY-148230
    TFEB Decoy ODN sodium
    		Inhibitor
    TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
    TFEB Decoy ODN sodium
  • HY-B2141
    Bendazol
    		Inhibitor 99.60%
    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-N0733R
    Glucosamine hydrochloride (Standard)
    		Inhibitor
    Glucosamine (hydrochloride) (Standard) is the analytical standard of Glucosamine (hydrochloride). This product is intended for research and analytical applications. 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 a dietary supplement. Glucosamine hydrochloride also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine hydrochloride (Standard)
  • HY-19949
    HIF-2α-IN-1
    		Inhibitor 99.94%
    HIF-2α-IN-1 (compound 9b) is a HIF-2α inhibitor (IC50=1.7 μM, SPA/scintillation proximity assay).
    HIF-2α-IN-1
  • HY-170522
    ISM012-042
    		Inhibitor 98.69%
    ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.
    ISM012-042
  • HY-177078
    Davotifan
    		Inhibitor
    Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer.
    Davotifan
  • HY-100947A
    cis VH-298
    		Inhibitor 99.96%
    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-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-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-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-183372
    HIF-IN-2
    		Inhibitor
    HIF-IN-2 is a HIF/HIF prolyl hydroxylase inhibitor. HIF-IN-2 suppresses HIF prolyl hydroxylase activity. HIF-IN-2 can be used for the research of anemia.
    HIF-IN-2
  • HY-403658
    IOX2-NH2
    		Inhibitor
    IOX2-NH2 (example 115) is a derivative of IOX2 (HY-15468). IOX2 is a chemical probe, and a specific prolyl hydroxylase-2 (PHD2) inhibitor.
    IOX2-NH2
  • 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-131346
    HIF-PHD-IN-1
    		Inhibitor 99.37%
    HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia.
    HIF-PHD-IN-1
  • HY-130264
    HIF-2α-IN-2
    		Inhibitor 99.93%
    HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
    HIF-2α-IN-2
  • HY-170915
    DDO-3055
    		Inhibitor 99.64%
    DDO-3055 is an orally active PHD2 inhibitor that can be used in the research of anemia associated with chronic kidney disease.
    DDO-3055
  • HY-151466
    HIF-1α-IN-5
    		Inhibitor 99.95%
    HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer.
    HIF-1α-IN-5
  • HY-N0390S7
    L-Glutamine-15N2,d5
    		Inhibitor 98%
    L-Glutamine-15N2,d5 is the deuterium and 15N-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na+-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.
    L-Glutamine-<sup>15</sup>N<sub>2</sub>,d<sub>5</sub>
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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