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-141510A
    myo-Inositol trispyrophosphate hexa-triethylamine
    		≥98.0%
    myo-Inositol trispyrophosphate (ITPP) hexa-triethylamine is a salt form of inositol triphosphate (ITPP). myo-Inositol trispyrophosphate hexa-triethylamine is a membrane-permeant hemoglobin allosteric regulator. myo-Inositol trispyrophosphate hexa-triethylamine enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. myo-Inositol trispyrophosphate hexa-triethylamine can be used in the study of cardiovascular disease and cancer.
    myo-Inositol trispyrophosphate hexa-triethylamine
  • HY-N0596R
    Panaxadiol (Standard)
    		Inhibitor
    Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
    Panaxadiol (Standard)
  • HY-161586
    Chloramphenicol/BSA
    		Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-P10426
    cyclo(CLLFVY)
    		Inhibitor
    cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers.
    cyclo(CLLFVY)
  • HY-161265
    HIF-2α agonist 3
    		Agonist
    HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with a EC50 value of 1.78 μM. HIF-2α agonist 3 can be used in the study of renal anemia.
    HIF-2α agonist 3
  • HY-P1888A
    HIF-1 alpha (556-574) (TFA)
    HIF-1 alpha (556-574) TFA 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) (TFA)
  • HY-B0988R
    Deferoxamine (mesylate) (Standard)
    		Activator
    Deferoxamine (mesylate) (Standard) is the analytical standard of Deferoxamine (mesylate). This product is intended for research and analytical applications. Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
    Deferoxamine (mesylate) (Standard)
  • HY-18259
    103D5R
    		Inhibitor
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM.
    103D5R
  • HY-170027
    LW1564
    		Inhibitor
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.
    LW1564
  • HY-170522
    ISM012-042
    		Inhibitor
    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-P10222
    Cyclo(CRLLIF)
    		Inhibitor
    Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively.
    Cyclo(CRLLIF)
  • HY-118672
    HNHA
    		Inhibitor 99.76%
    HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer.
    HNHA
  • HY-147813
    HIF-1α-IN-3
    		Inhibitor
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency.
    HIF-1α-IN-3
  • HY-163601
    HIF-2α-IN-14
    		Inhibitor
    HIF-2α-IN-14 (18) is a HIF-2α inhibitor, with an IC50 of 0.27 μM.
    HIF-2α-IN-14
  • HY-N0234R
    Bavachinin (Standard)
    		Inhibitor
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..
    Bavachinin (Standard)
  • HY-163598
    HIF-2α-IN-11
    		Inhibitor
    HIF-2α-IN-11 (1) is a HIF-2α inhibitor, with an IC50 of 59.2 nM.
    HIF-2α-IN-11
  • HY-144332
    PHD2/HDACs-IN-1
    		Inhibitor
    PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI).
    PHD2/HDACs-IN-1
  • HY-12519S
    Oltipraz-d3
    		Inhibitor
    Oltipraz-d3 is the deuterium labeled Oltipraz. 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. Oltipraz is a potent Nrf2 activator.
    Oltipraz-d<sub>3</sub>
  • HY-161427
    HSP90-IN-30
    		Inhibitor
    HSP90-IN-30 (compound 3e) inhibits HSP90 chaperone activity. HSP90-IN-30 inhibits the activity of HIF-1 transcriptional under hypoxia with an IC50 value of 2.16 μM.
    HSP90-IN-30
  • HY-15468A
    IOX2 sodium
    		Inhibitor
    IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases.
    IOX2 sodium
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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