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-B0230A
    Thiazolinobutazone
    		Inhibitor
    Thiazolinobutazone is a COX inhibitor. Thiazolinobutazone has less toxic than Phenylbutazone (HY-B0230). Thiazolinobutazone can be used in the study of immunological diseases.
    Thiazolinobutazone
  • HY-N4044
    Hirsutanonol
    		Inhibitor
    Hirsutanonol ((5S)-Hirsutanonol) is a diarylheptanoid that can be isolated from the bark of Alnus hirsute var. sibirica. Hirsutanonol inhibits cyclooxygenase-2 (COX-2) expression. Hirsutanonol has anti-filarial with an IC50 value of 44.11 μg/mL for microfilariae.
    Hirsutanonol
  • HY-17372S
    Rofecoxib-d5
    		Inhibitor
    Rofecoxib-d5 is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
    Rofecoxib-d<sub>5</sub>
  • HY-B0905AR
    Tilmicosin phosphate (Standard)
    		Inhibitor
    Tilmicosin (phosphate) (Standard) is the analytical standard of Tilmicosin (phosphate). This product is intended for research and analytical applications. Tilmicosin (LY-177370) phosphate is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin phosphate mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin phosphate is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin phosphate has immunomodulatory and anti-inflammatory effects[1][2][3][4][5][6].
    Tilmicosin phosphate (Standard)
  • HY-152120
    (±)-Aiphanol
    		Inhibitor
    (±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak.(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 μM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active.
    (±)-Aiphanol
  • HY-105579
    Isonixin
    		Inhibitor
    Isonixin (Isonixine) is a non-steroidal compound. Isonixin can be used for the research of pain and inflammation.
    Isonixin
  • HY-117019
    LY150310 free base
    		Inhibitor
    LY150310 inhibits thromboxane synthase, cyclooxygenase, and thrombin activation. LY150310 inhibits spontaneous lung metastasis in a dose-dependent manner.
    LY150310 free base
  • HY-N10782
    Balanophonin
    		Inhibitor
    Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis.
    Balanophonin
  • HY-146370
    COX-2-IN-12
    		Inhibitor
    COX-2-IN-12 (compound 3b) is a potent and selective inhibitor of COX-2 with an IC50 of 19.98 μM. COX-2-IN-12 is an anti-inflammatory agent. COX-2-IN-12 shows safety in-vivo acute toxicity study.
    COX-2-IN-12
  • HY-162168
    Anti-inflammatory agent 71
    		Inhibitor
    Anti-inflammatory agent 71 (Compound 3.2) is an anti-inflammatory agent that can reduce the levels of neutrophils, COX-2, nitrotyrosine, IL-1b, and C-reactive protein, while increasing the level of eNOS.
    Anti-inflammatory agent 71
  • HY-115920
    Anti-inflammatory agent 8
    Anti-inflammatory agent 8 (compound 13) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 8 expresses activity on COX-2 enzyme more than COX-1 with an IC50 of 0.09 nM. Anti-inflammatory agent 8 is orally active.
    Anti-inflammatory agent 8
  • HY-170836
    NLRP3-IN-69
    		Inhibitor
    NLRP3-IN-69 (Compound 23) inhibits the activation of NF-κB p65 and the formation of NLRP3 inflammasome. NLRP3-IN-69 inhibits LPS (HY-D1056)-induced overexpression of IL-1β, iNOS and COX-2, inhibits NO generation (IC50=5.66 μM), thereby exhibiting anti-inflammatory activity.
    NLRP3-IN-69
  • HY-159516
    Sabialimon P
    		Inhibitor
    Sabialimon P (compound 16) is a NO release inhibitor (IC50=18.12 μM) with anti-inflammatory activity. Sabialimon P significantly reduces the secretion of TNF-α, iNOS, IL-6 and NF-κB and inhibits the expression of COX-2 and NF-κB/p65 in RAW264.7 cells induced by LPS (HY-D1056).
    Sabialimon P
  • HY-P10710
    BMP-4
    		Inhibitor
    BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms.
    BMP-4
  • HY-N3555
    (+)-Catechin pentaacetate
    		Inhibitor
    (+)-Catechin pentaacetate is a precursor for the production of (+) catechin (HY-N0898 ). (+) catechin is a useful natural herbicide and antimicrobial. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
    (+)-Catechin pentaacetate
  • HY-147961
    COX-2-IN-23
    		Inhibitor
    COX-2-IN-23 (compound 9a) is a selective COX-2 inhibitor with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1. COX-2-IN-23 has anti-inflammatory activity and low ulcerogenic activity.
    COX-2-IN-23
  • HY-146419
    Anti-inflammatory agent 20
    		Inhibitor
    Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation.
    Anti-inflammatory agent 20
  • HY-12383S
    Pelubiprofen-13C,d3
    		Inhibitor
    Pelubiprofen-13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
    Pelubiprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-121679
    COX-2-IN-50
    		Inhibitor
    COX-2-IN-50 is a water-soluble COX-2 inhibitor with significant analgesic activity. The solubility of COX-2-IN-50 in water reaches 20.3 mg/mL, far exceeding the 1.6 μg/mL of its precursor compound PC407. COX-2-IN-50 demonstrates good biocompatibility and is suitable for the development of injectable dosage forms. COX-2-IN-50 has proven its analgesic effect in vivo and shows potential application value.
    COX-2-IN-50
  • HY-106050
    Tilomisole
    		Inhibitor
    Tilomisole (Wy 18251) is a benzimidazothiazole experimental agent with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation.
    Tilomisole
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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