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-B1398
    Ampyrone
    		Inhibitor 99.72%
    Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy.
    Ampyrone
  • HY-B0476S
    Phenacetin-d5
    		Inhibitor 99.51%
    Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats.
    Phenacetin-d<sub>5</sub>
  • HY-15321S
    Etoricoxib-d4
    		98.82%
    Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib-d<sub>4</sub>
  • HY-N7012
    7,3',4'-Tri-O-methylluteolin
    		Inhibitor 99.28%
    7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activitiessup>[4]sup>[5].
    7,3',4'-Tri-O-methylluteolin
  • HY-W012399
    2,5-Di-tert-butylhydroquinone
    		Modulator 99.90%
    2,5-Di-tert-butylhydroquinone (BHQ) (Compound 2), an indirect food additive, is a Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor with an IC50 of 400 nM. 2,5-Di-tert-butylhydroquinone disrupts the gating function of the residue Glu309 which prevents Ca2+ from reaching their binding site. 2,5-Di-tert-butylhydroquinone regulates the activity of 5-lipoxygenase and COX-2 (IC50: 1.8 and 14.1 μM for 5-LO and COX-2, respectively).
    2,5-Di-tert-butylhydroquinone
  • HY-17479A
    Amfenac Sodium Hydrate
    		Inhibitor 99.07%
    Amfenac Sodium Hydrate is a COX-2 inhibitor.
    Amfenac Sodium Hydrate
  • HY-N2459
    Peonidin chloride
    		Inhibitor 98.70%
    Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
    Peonidin chloride
  • HY-129113
    α-​Chaconine
    		Inhibitor 99.76%
    α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
    α-​Chaconine
  • HY-N2429
    Sphondin
    		Inhibitor 99.70%
    Sphondin possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells.
    Sphondin
  • HY-N0001R
    (-)-Epicatechin (Standard)
    		Inhibitor
    (-)-Epicatechin (Standard) is the analytical standard of (-)-Epicatechin. This product is intended for research and analytical applications. (-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
    (-)-Epicatechin (Standard)
  • HY-131258
    Ibuprofen impurity 1
    		Inhibitor
    Ibuprofen impurity 1 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 1
  • HY-Y0543
    5-Methylfurfural
    		99.96%
    5-Methylfurfural is a chemical that can be utilized as food additive, intermediate in the production of agrochemicals, and precursor of certain anti-cancer natural products. 5-Methylfurfural is formed during the photoexposition of ranitidine hydrochloride. 5-Methylfurfural is an organic compound. 5-Methylfurfural has a strong tendency to be further hydrogenated to 2,5-dimethylfuran (DMF). 5-Methylfurfural can predominantly evoke skin inflammation and barrier disintegration. 5-Methylfurfural degrades native DNA through the formation of single-strand breaks.
    5-Methylfurfural
  • HY-17357S
    Nepafenac-d5
    		Inhibitor 98.84%
    Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
    Nepafenac-d<sub>5</sub>
  • HY-N7064
    Iminostilbene
    		Inhibitor 99.34%
    Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
    Iminostilbene
  • HY-113445
    Thromboxane B3
    Thromboxane B3 is a prostaglandin analog derived from arachidonic acid (AA) in the cyclooxygenase (COX) metabolic pathway. Thromboxane B3 is generated from arachidonic acid (AA) in platelets and vascular endothelial cells through the catalysis of cyclooxygenase (COX) and thromboxane synthase (TXS). Thromboxane B3 has been reported to be formed by human platelets upon ingestion of eicosapentaenoic acid (C20: 5ω3).
    Thromboxane B3
  • HY-W011849
    Phenyl β-D-glucopyranoside
    		Inhibitor 99.85%
    Phenyl β-D-glucopyranoside has anti-cancer and anti-inflammatory activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB.
    Phenyl β-D-glucopyranoside
  • HY-W012817
    Methylhydroquinone
    		Inhibitor 99.88%
    Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions.
    Methylhydroquinone
  • HY-14654S1
    Aspirin-d4
    		Inhibitor
    Aspirin-d4 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin-d<sub>4</sub>
  • HY-17361
    Etofenamate
    		Inhibitor 98.35%
    Etofenamate, a non-steroid anti-inflammatory agent (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases.
    Etofenamate
  • HY-N1731
    2′-Hydroxy-5′-methoxyacetophenone
    		Inhibitor 99.96%
    2'-Hydroxy-5'-methoxyacetophenone is an acetophenone derivative with acaricidal activities. 2'-Hydroxy-5'-methoxyacetophenone attenuates the inflammatory response via NF-κB signaling pathway. 2'-Hydroxy-5'-methoxyacetophenone exhibits significant inhibitory activity against α-amylase, collagenase and aldose reductase (AR) with IC50s of 0.928, 3.264 and 20.046 μM, highlighting its potential in combating diabetes. 2'-Hydroxy-5'-methoxyacetophenone exhibits anti-ovarian cancer activity.
    2′-Hydroxy-5′-methoxyacetophenone
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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