2. Signaling Pathways
  3. Immunology/Inflammation
  4. COX

COX

Cyclooxygenase

COX

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Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).

COX Isoform Specific Products:

COX Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-105028S
    Tenidap-d3
    		Inhibitor
    Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
    Tenidap-d<sub>3</sub>
  • HY-181156
    Anti-inflammatory agent 112
    		Inhibitor
    Anti-inflammatory agent 112 is an inducible nitric oxide synthase (iNOS) inhibitor, a COX-2 inhibitor, and an anti-inflammatory agent. Anti-inflammatory agent 112 suppresses i-NOS and COX-2 protein expression, reduces nitric oxide, IL-6, and TNF-α production, and attenuates lipopolysaccharide (LPS)-induced inflammatory responses. Anti-inflammatory agent 112 can be used for the research of inflammatory disorders.
    Anti-inflammatory agent 112
  • HY-W040045R
    Callistephin chloride (Standard)
    		Inhibitor
    Callistephin (Pelargonidin 3-O-glucoside) chloride (Standard) is the analytical standard of Callistephin chloride (HY-W040045). This product is intended for research and analytical applications. Callistephin chloride is an anthocyanin. Callistephin chloride regulates the expression of inflammatory (reducing iNOS/TNF-α/COX-2) and apoptosis-related proteins by inhibiting p38 phosphorylation, and enhances the protective effect of Isoflurane (HY-A0134) on microglial cell damage. Callistephin chloride significantly reduces ROS levels, eliminates DPPH free radicals, protects retinal pigment epithelial cells, and inhibits lipid peroxidation. Callistephin chloride can alleviate glutamate excitotoxicity, reduce neuronal apoptosis, and protect cerebellar granule neurons. Callistephin chloride can inhibit the proliferation and metastasis of breast cancer cells by inducing apoptosis.
    Callistephin chloride (Standard)
  • HY-178440
    EGFR/COX-2-IN-2
    		Inhibitor
    EGFR/COX-2-IN-2 (Compound 10a) is a dual inhibitor targeting epidermal growth factor receptor (EGFR) (IC50= 6.0 μM) and cyclooxygenase-2 (COX-2) (IC50=50 μM). EGFR/COX-2-IN-2 induces S-phase cell cycle arrest and apoptosis. EGFR/COX-2-IN-2 is promising for research of cancers and inflammation-related diseases.
    EGFR/COX-2-IN-2
  • HY-116763
    COX-2/5-LOX-IN-4
    		Inhibitor
    COX-2/5-LOX-IN-4 (Compound 1) is a dual inhibitor that acts on both COX-2 and 5-LOX, with IC50 values of 0.05 μM for COX-2 and 0.003 μM for 5-LOX. By inhibiting the arachidonic acid metabolism pathway, COX-2/5-LOX-IN-4 reduces the production of prostaglandins and leukotrienes, alleviating inflammatory responses. In a rat ear edema model, intravenous administration (0.01 and 0.1 mg/kg) reduced edema by 41% and 44%, respectively, demonstrating significant anti-inflammatory effects. COX-2/5-LOX-IN-4 shows promise for studying the mechanisms of inflammatory diseases.
    COX-2/5-LOX-IN-4
  • HY-173114
    Anti-inflammatory agent 96
    Anti-inflammatory agent 96 (Compound 5), a tetrasubstituted α-aminophosphonate derivatives with a methylphosphoserine fragment, is an anti-inflammatory agent. Anti-inflammatory agent 96 can reduce TPA-induced ear edema and CFA-induced paw edema.
    Anti-inflammatory agent 96
  • HY-135081
    N-(4-acetamidophenyl)-Indomethacin amide
    		Inhibitor
    N-(4-acetamidophenyl)-indomethacin amide (N-4-AIA) is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2.1 N-4-AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.12 and 0.625 μM, respectively. It is about 400 times less potent as an inhibitor of human recombinant COX-1 and 80 times less potent as an inhibitor of ovine COX-1 than ovine COX-2.
    N-(4-acetamidophenyl)-Indomethacin amide
  • HY-126121
    2-Hydroxy Ibuprofen
    		Inhibitor
    2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
    2-Hydroxy Ibuprofen
  • HY-155808
    STAT3-IN-18
    		Inhibitor
    STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
    STAT3-IN-18
  • HY-101579
    LY 178002
    		Inhibitor 99.60%
    LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
    LY 178002
  • HY-101670
    MTPPA
    		Inhibitor 99.82%
    MTPPA is a agent for treating symptoms of inflammation and pain.
    MTPPA
  • HY-180829
    HDAC6-IN-71
    		Inhibitor
    HDAC6-IN-71 (Compound 24) is a HDAC6 inhibitor with IC50 values for HDAC6 and HDAC1 of 13.68 and 443.12 nM respectively. HDAC6-IN-71 effectively inhibits the production of NO by mouse macrophages, with its IC50 being 2.31 μM. HDAC6-IN-71 inhibits the HDAC6-NF-κB signaling pathway, reduces the levels of phosphorylated IκB-α and IKK-α/β, and suppresses the expression of downstream inflammatory proteins COX-2 and iNOS. HDAC6-IN-71 significantly alleviates ulcerative colitis in mice.
    HDAC6-IN-71
  • HY-134521
    Diclofenac amide
    		Inhibitor
    Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg).
    Diclofenac amide
  • HY-N11784
    Triptolidenol
    		Inhibitor
    Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research.
    Triptolidenol
  • HY-181273
    COX-2/5-LOX-IN-7
    		Inhibitor
    COX-2/5-LOX-IN-7 (Hybrids 9) is a COX-2 (IC50 = 3.3 μM)/5-LOX (IC50 = 3.1 μM) inhibitor. COX-2/5-LOX-IN-7 can be used in research on diseases such as inflammation.
    COX-2/5-LOX-IN-7
  • HY-173115
    15-LOX-IN-2
    		Inhibitor
    15-LOX-IN-2 (Compound 2a) is an orally active COX-2/15-LOX inhibitor and a partial agonist of PPARγ. 15-LOX-IN-2 has anti-inflammatory activity and inhibits the levels of 20-HETE, IL-1β and TNF-α in RAW 264.7 cells treated with LPS (HY-D1056). In addition, 15-LOX-IN-2 has significant glucose uptake capacity in the absence of insulin. 15-LOX-IN-2 can be used for the research of metabolic diseases.
    15-LOX-IN-2
  • HY-179700
    COX-2-IN-61
    		Inhibitor
    COX-2-IN-61 is an orally active COX-2 inhibitor with an IC50 of 22 µM, also inhibits COX-1 with an IC50 of 43 µM. COX-2-IN-61 exhibits anti-inflammation effects in a Carrageenan (HY-125474) induced rat paw edema model, with promising safety profiles. COX-2-IN-61 can be used for the research of inflammation.
    COX-2-IN-61
  • HY-W676872
    Dihydroflavokawin B
    		Inhibitor
    Dihydroflavokawin B is a selective COX-1 inhibitor with an IC50 of 1.22 μM. Dihydroflavokawin B weakly inhibits COX-2 and 5-LOX. Dihydroflavokawin B inhibits promastigote forms of Leishmania panamensis and Leishmania braziliensis. Dihydroflavokawin B inhibits rabbit platelet aggregation induced by Arachidonic acid, platelet activating factor, and adenosine diphosphate. Dihydroflavokawin B exhibits in vitro anti-inflammatory activity. Dihydroflavokawin B can be used for the research of leishmaniasis.
    Dihydroflavokawin B
  • HY-182291
    COX-1/2-IN-11
    		Inhibitor
    COX-1/2-IN-11 is a dual inhibitor of COX-1 and COX-2, with an IC50 of 345 nM against COX-1. COX-1/2-IN-11 can be used in the development of non-steroidal anti-inflammatory agents.
    COX-1/2-IN-11
  • HY-17487
    Miroprofen
    		Inhibitor
    Miroprofen (Y 0213) is an orally active nonsteroidal anti-inflammatory analgesic (NSAID). Miroprofen exhibits anti-inflammatory, analgesic and anti-platelet activities.
    Miroprofen
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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