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-P10797
    TAT-N24
    		Inhibitor
    TAT-N24 is a cell-permeable TAT peptide as a p55PIK signaling inhibitor. TAT-N24 is effective for corneal neovascularization (CNV) and ocular inflammation by inhibiting the HIF-1α/NF-κB signaling pathway in corneal suture (CS). TAT-N24 also inhibits corneal neovascularization.
    TAT-N24
  • HY-14575
    Nastorazepide hemicalcium
    		Inhibitor
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide hemicalcium
  • HY-134998
    Oltipraz metabolite M2
    		Inhibitor
    Oltipraz metabolite M2, an active metabolite of Oltipraz (HY-12519), is an orally active HIF-1α inhibitor. Oltipraz metabolite M2 increases mitochondrial fuel oxidation and inhibits lipogenesis in the liver by dually activating AMPK in high-fat diet (HFD)-fed mice. Oltipraz metabolite M2 can be used for hepatic steatosis and steatohepatitis research.
    Oltipraz metabolite M2
  • HY-163839
    DS-1093a
    		Inhibitor
    DS-1093a is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitor, with an EC50 of 0.49 μM in Hep3B cell EPO production. DS-1093a can be used in the research of renal anemia.
    DS-1093a
  • HY-155009
    PHD2-IN-1
    		Inhibitor
    PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research.
    PHD2-IN-1
  • HY-N0242R
    Fraxinellone (Standard)
    		Inhibitor
    Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
    Fraxinellone (Standard)
  • HY-157444
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG
    		Inhibitor
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) is a potent adjuvant obtained by optimization of the structure of EGCG. 5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) decreases the expression of HIF-1α and CBR1 at both the mRNA and protein levels.
    5,3',4',3'',4'',5''-6-O-Ethyl-EGCG
  • HY-177271
    PHD2-IN-6
    		Inhibitor
    PHD2-IN-6 (Example 89) is a HIF prolyl hydroxylase 2 (PHD2) inhibitor with an IC50 of 31.6  nM. PHD2-IN-6 stimulates encoding erythropoietin (EPO) production. PHD2-IN-6 can be used for inflammatory diseases like inflammatory bowel disease (IBD) and rheumatoid arthritis research.
    PHD2-IN-6
  • HY-W800535
    Cryptolepine
    		Inhibitor
    Cryptolepine is an orally active multi-potent alkaloid with anti-cancer, anti-bacterial, anti-viral, anti-malarial, anti-inflammatory, anti-hyperglycemic, relieve pain and other properties. Cryptolepine acts as an inhibitor of c-Myc, mTOR, NF-κB, HIF-1, MAPK and an activator of AMPKα1/2. It intercalates into DNA, inhibits topoisomerase II (Top II), disrupts mitochondrial dynamics and induces apoptosis. Cryptolepine also exhibits anti-plasmodial and cholinesterase inhibitory activities. Cryptolepine can be used in research related to tumors (melanoma, hepatocellular carcinoma, mammary adenocarcinoma, etc.), malaria, inflammatory diseases and diabetes, particularly in studies focused on inhibiting tumor growth and anti-plasmodial infection.
    Cryptolepine
  • HY-B1125R
    Glucosamine (Standard)
    		Inhibitor
    Isomogroside V (Standard) is the analytical standard of Isomogroside V. This product is intended for research and analytical applications. Isomogroside V is a sweetener, which extracted from Siraitia grosvenorii (Swingle).
    Glucosamine (Standard)
  • HY-129502
    Fibrostatin C
    		Inhibitor
    Fibrostatin C (P-23924C) is an orally active prolyl hydroxylase inhibitor that also inhibits collagen biosynthesis. Fibrostatin C also increases the number of cytoplasmic granules immunoreactive with antibodies to collagen I or III. Fibrostatin C inhibits the secretion of type I collagen in Tenon's capsule fibroblasts. Fibrostatin C is promising for research of the wound fibrotic response in the wound of glaucoma filtering surgery.
    Fibrostatin C
  • HY-175521
    HIF-1α-IN-8
    		Inhibitor
    HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).
    HIF-1α-IN-8
  • HY-165413
    KST012174 hydrochloride
    		Inhibitor
    KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC50 of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies.
    KST012174 hydrochloride
  • HY-153513
    PHD-1-IN-4
    		Inhibitor 99.94%
    PHD-1-IN-4 is a brain-penetrant PHD-1 inhibitor with an IC50 of 0.074 μM.
    PHD-1-IN-4
  • HY-163148
    PHD-IN-3
    		Inhibitor
    PHD-IN-3 (Compound 15) is an orally active PHD inhibitor. PHD-IN-3 can be used in the study of anemia associated with chronic kidney disease.
    PHD-IN-3
  • HY-163512
    Anti-inflammatory agent 79
    		Inhibitor
    Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.
    Anti-inflammatory agent 79
  • HY-141625A
    TRC160334 sodium
    		Inhibitor
    TRC160334 sodium is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 sodium can be used for the research of ischemia/reperfusion injury.
    TRC160334 sodium
  • HY-163600
    HIF-2α-IN-13
    		Inhibitor
    HIF-2α-IN-13 (18) is a HIF-2α inhibitor, with an IC50 of 2.7 μM.
    HIF-2α-IN-13
  • HY-179434
    HIF-1α-IN-10
    		Inhibitor
    HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2 (HY-179424).
    HIF-1α-IN-10
  • HY-179341
    CHNQD-03301
    		Inhibitor
    CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC50 = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer.
    CHNQD-03301
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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