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-155159
    COX-2/15-LOX-IN-2
    		Inhibitor
    COX-2/15-LOX-IN-2 is a potent dual COX-2 and 15-LOX inhibitor with IC50 values of 0.065?μM and 1.86?μM, respectively. COX-2/15-LOX-IN-2 has potent antioxidant activity.
    COX-2/15-LOX-IN-2
  • HY-175643
    COX-2-IN-58
    		Inhibitor
    COX-2-IN-58 is a COX-2 inhibitor. COX-2-IN-58 exhibits remarkable anti-inflammatory activity in Carrageenan (HY-125474)-induced paw edema model of Balb/C mice. COX-2-IN-58 can be used for the research of inflammation.
    COX-2-IN-58
  • HY-N7630
    Rehmapicrogenin
    		Inhibitor
    Rehmapicrogenin, isolated from the root of Rehmannia glutinosa, exhibits potent anti-inflammatory effect by inhibiting iNOS, COX-2 and IL-6.
    Rehmapicrogenin
  • HY-167734
    Pemedolac
    		Inhibitor
    Pemedolac (AY-30715) is a potent analgesic with significant pain-relief efficacy against chemically induced and inflammatory pain in animal models. Pemedolac displays a notable separation between analgesic effects and anti-inflammatory activity, achieving effective pain relief at much lower doses than those required for anti-inflammatory or gastric irritant effects. Pemedolac also shows low ulcerogenic potential, indicating a safer profile compared to standard NSAIDs while being utilized for the treatment of neurological, skin, and musculoskeletal disorders.
    Pemedolac
  • HY-N0043R
    Ginsenoside Rd (Standard)
    		Inhibitor
    Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
    Ginsenoside Rd (Standard)
  • HY-157127
    Ketoprofen L-thyroxine ester
    		Inhibitor
    Ketoprofen L-thyroxine ester is a prodrug of Ketoprofen. Ketoprofen L-thyroxine ester reservoir and release ketoprofen slowly in the brain.
    Ketoprofen L-thyroxine ester
  • HY-147811
    Heterophdoid A
    		Inhibitor
    Heterophdoid A (Compound 1) is an anti-inflammatory agent. Heterophdoid A inhibits NO production with an IC50 of 5.93 μM in BV-2 cells.
    Heterophdoid A
  • HY-172402
    Vasoactive intestinal peptide
    		Activator
    Vasoactive intestinal peptide is an agonist of VPAC1/VPAC2 receptor (G-protein-coupled receptors). Vasoactive intestinal peptide reduces corneal perforation rate, bacterial load, and excessive neutrophil infiltration in Pseudomonas aeruginosa-induced keratitis models. Vasoactive intestinal peptide enhances anti-inflammatory mediators like IL-10 and TGF-β, inhibites pro-inflammatory factors such as IL-1β and TNF-α, and upregulates lipid mediator-related enzymes (SOCS3, COX-2, ALOX12) to promote inflammation resolution. Vasoactive intestinal peptide is promising for research of ocular infectious diseases.
    Vasoactive intestinal peptide
  • HY-161994
    COX-2-IN-47
    		Inhibitor
    COX-2-IN-47 (compound 6c ) is a selective COX-2 inhibitor with IC50 value of 0.03 μM. COX-2-IN-47 has antiedema activity.
    COX-2-IN-47
  • HY-121996
    Prostaglandin E2 Ethanolamide
    Prostaglandin E2 Ethanolamide (PGE2-EA), an analog of PGE2, can be formed enzymatically following COX-2 oxygenation of endocannabinoids. Prostaglandin E2 Ethanolamide (PGE2-EA) could modulate the production of the proinflammatory cytokine TNF-α in human blood and human monocytic cells.
    Prostaglandin E2 Ethanolamide
  • HY-N1380S
    Guaiacol-d7
    Guaiacol-d7 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
    Guaiacol-d<sub>7</sub>
  • HY-N0147R
    Rutaecarpine (Standard)
    		Inhibitor
    Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM.
    Rutaecarpine (Standard)
  • HY-161513
    iNOS/COX-2-IN-1
    		Inhibitor
    iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects.
    iNOS/COX-2-IN-1
  • HY-N13040
    Isoscoparin-7-O-glucoside
    		Inhibitor
    Isoscoparin-7-O-glucoside is a flavonoid compound found in barley leaves. The total phenolic content (TPC) of isoscoparin-7-O-glucoside is positively correlated with COX-2 inhibitory activity, indicating anti-inflammatory activity. Isoscoparin-7-O-glucoside can be used in the study of inflammation.
    Isoscoparin-7-O-glucoside
  • HY-W741411
    Tenoxicam-d4
    Tenoxicam-d4 (Ro-12-0068-d4) is the deuterium labeled Tenoxicam (HY-B0440). Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
    Tenoxicam-d<sub>4</sub>
  • HY-115966
    COX-1/2-IN-1
    		Inhibitor
    COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively.
    COX-1/2-IN-1
  • HY-173518
    SIN 14
    		Inhibitor
    SIN 14, a derivative of Sinomenine (HY-15122), is an orally active HO-1 activator (KD = 17.2 μM). SIN 14 binds to the catalytic core domain of HO-1 and induces HO-1 activation in catalysis. SIN 14 significantly increases HO-1 stability. SIN 14 has anti-inflammatory effects and inhibits M1 macrophage polarization while promoting M2 polarization in LPS (Lipopolysaccharides)(HY-D1056)-induced RAW264.7 cells. SIN 14 inhibits inflammatory mediator production (eg: NO, IL-6, IL-1β and CCL2, inhibits production of ROS and down-regulates the expression of COX-2 and iNOS. SIN 14 can inhibit RA-related inflammatory edema in collagen-induced arthritis (ClA) mice.
    SIN 14
  • HY-159562
    COX-2-IN-46
    		Inhibitor
    COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM).
    COX-2-IN-46
  • HY-149270
    COX-2-IN-31
    		Inhibitor
    COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity.
    COX-2-IN-31
  • HY-N16129
    Diplacone
    		Inhibitor
    Diplacone (DP) is a geranylated flavanone. Diplacone can be isolated from the unripe fruits of Paulownia tomentosa. Diplacone has anti-inflammatory, antiradical, cytoprotective, antibacterial and anticancer activities. Diplacone induces ferroptosis-mediated cell death by increasing mitochondrial Ca2+ Influx, ROS production and mitochondrial permeability transition. Diplacone significantly inhibits AChE and BChE activity with IC50s of 7.2  μM and 1.4 μM for hAChE and BChE, respectively. Diplacone can be used for chronic inflammatory diseases like inflammatory bowel diseases (IBD), cancers like lung cancer and Alzheimer’s disease research.
    Diplacone
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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