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-131260
    Ibuprofen Impurity K
    		Inhibitor
    Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
    Ibuprofen Impurity K
  • HY-66005S3
    Acetaminophen-13C6
    		Inhibitor
    Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
    Acetaminophen-<sup>13</sup>C<sub>6</sub>
  • HY-B0440S
    Tenoxicam-d3
    		Inhibitor
    Tenoxicam-d3 is the deuterium labeled Tenoxicam. Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
    Tenoxicam-d<sub>3</sub>
  • HY-181061
    COX/5-LO-IN-2
    		Inhibitor
    COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.
    COX/5-LO-IN-2
  • HY-N4314R
    Scutellarein tetramethyl ether (Standard)
    		Inhibitor
    Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL).
    Scutellarein tetramethyl ether (Standard)
  • HY-162385
    COX-2-IN-42
    		Inhibitor
    COX-2-IN-42 (Compound T1) is a COX-2 inhibitor, and protects zebrafish against PTZ-induced neuronal damage.
    COX-2-IN-42
  • 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-W747297
    β-Selinene
    		Inhibitor
    β-Selinene is a sesquiterpene and is the main active component of the essential oil of red purple hibiscus (Callicarpa macrophylla). β-Selinene exhibits significant related antioxidant activity, anti-inflammatory activity, and antipyretic analgesic activity. β-Selinene may exert antioxidant effects by directly scavenging free radicals (DPPH, NO, •OH) and chelating pro-oxidative metal ions (Fe²⁺); inhibit cyclooxygenase (COX) activity, reduce prostaglandin (such as PGE₂) synthesis to exert anti-inflammatory effects; regulate the thermoregulatory set point of the hypothalamus and inhibit inflammatory mediators to exert antipyretic and analgesic effects.
    β-Selinene
  • HY-181044
    COX-2/5-LOX-IN-6
    		Inhibitor
    COX-2/5-LOX-IN-6 (Compound 4c) is a potent and selective 5-LOX (IC50 = 0.10 μM) and COX-2 (IC50: 2.88 μM) inhibitor. COX-2/5-LOX-IN-6 displays potent anticancer activity against ovarian cancer. COX-2/5-LOX-IN-6 would not cause cytotoxic effects in noncancerous cells. COX-2/5-LOX-IN-6 is a potential anti-inflammatory agent.
    COX-2/5-LOX-IN-6
  • 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.
    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-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
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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