COX
Cyclooxygenase (COX) catalyzes the conversion of arachidonic acid into prostaglandin G2 and prostaglandin H2, initiating prostanoid biosynthesis that regulates inflammation, vascular homeostasis, pain signaling, and tissue responses to injury[1][2]. Mechanistically, COX enzymes contain two major isoforms, COX-1 and COX-2, which catalyze the same biochemical reaction but differ in gene regulation, tissue distribution, intracellular localization, and substrate selectivity[1][2]. COX-1 is constitutively expressed in most tissues and contributes to gastric mucosal protection, platelet function, and renal hemodynamic maintenance, whereas COX-2 is rapidly induced by inflammatory cytokines, growth factors, and pathological stimuli[1][3]. In disease models, increased COX-2 expression is associated with chronic inflammatory disorders, neurodegenerative diseases, and multiple cancer types, supporting its central role in inflammation-driven pathophysiology and tumor progression[1][2]. Compared with related isoforms, COX-2 contains a larger and more flexible substrate-binding channel that enables distinct inhibitor selectivity and broader fatty-acid utilization[1][4]. Therefore, selective and non-selective nonsteroidal anti-inflammatory drugs (NSAIDs) remain important experimental tools for dissecting prostaglandin-dependent signaling pathways, while COX-2-selective inhibitors have been widely used to investigate inflammatory mechanisms and disease-associated prostanoid production[1][2][4].
References:
- [1]. Faki Y, et al. Different Chemical Structures and Physiological/Pathological Roles of Cyclooxygenases. Rambam Maimonides Med J. 2021 Jan 19;12(1):e0003. [Content Brief]
- [2]. Joanne P, et al. Lipid reorganization induced by membrane-active peptides probed using differential scanning calorimetry. Biochim Biophys Acta. 2009 Sep;1788(9):1772-81. [Content Brief]
- [3]. Cyclooxygenase in sciencedirect topic.
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COX Related Products (740)
Related Products (740)
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Asaraldehyde (Standard)
0 ImagesSynonyms: Asaronaldehyde (Standard); 2,4,5-trimethoxy-Benzaldehyde (Standard)Asaraldehyde (Standard) is the analytical standard of Asaraldehyde. This product is intended for research and analytical applications. Asarylaldehyde (Asaronaldehyde), a COX-2 inhibitor, significantly inhibits cyclooxygenase II (COX-2) activity with an IC50 value of 100 μg/mL.
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COX-2-IN-36
0 ImagesCat. No.: HY-105304CAS No.: 189954-93-6COX-2-IN-36 (compound 1) is a very potent and specific COX-2 inhibitor, with an IC50 of 0.4 μM.
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Mefenamic Acid-d3
0 ImagesCat. No.: HY-B0574S1CAS No.: 1189707-81-0Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a BBB-permeable non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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N-(3-Pyridyl)indomethacinamide
0 ImagesCat. No.: HY-139129CAS No.: 261766-29-4N-(3-Pyridyl)indomethacinamide is a derivative of Indomethacin (HY-14397). N-(3-Pyridyl)indomethacinamide is a COX2 inhibitor.
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6-Hydroxy etodolac
0 ImagesCat. No.: HY-139433CAS No.: 101901-06-86-Hydroxy etodolac (compound 2) is a metabolite of Etodolac (HY-76251). Etodolac is a non-steroidal anti-inflammatory compound and is a COX inhibitor.
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Fenofibric acid-13C8
0 ImagesCat. No.: HY-B0760S1Synonyms: FNF acid-13C8Fenofibric acid-13C8 (FNF acid-13C8) is 13C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
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KME-4
0 ImagesCat. No.: HY-19014CAS No.: 83677-24-1KME-4 is an orally active dual inhibitor of 5-lipoxygenase (5-lipoxygenase) and cyclooxygenase (cyclooxygenase). KME-4 inhibits 5-lipoxygenase in the cytosol of guinea pig polymorphonuclear leukocytes (PMNL) and cyclooxygenase in rabbit platelets, with IC50 values of 0.85 μM and 0.44 μM, respectively. KME-4 can be used in studies related to arachidonic acid metabolism, inflammatory responses, and arthritis.
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Lotifazole
0 ImagesCat. No.: HY-119167CAS No.: 71119-10-3Synonyms: F 1686Lotifazole (F 1686) is a non-steroidal anti-inflammatory agent. Lotifazole exhibits specific inhibition of delayed-type hypersensitivity and does not rely on the prostaglandin synthesis inhibition pathway at low doses. Lotifazole shows significant efficacy in treating paw edema induced by carrageenan in rats, erythema induced by ultraviolet radiation in guinea pigs, and pleurisy at high doses. Lotifazole can be used for the study of T-cell-mediated diseases.
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5'-Hydroxy meloxicam
0 ImagesCat. No.: HY-124351CAS No.: 130262-92-9
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Naproxen-d3
0 ImagesCat. No.: HY-15030S1CAS No.: 1094102-82-5Synonyms: (S)-Naproxen-d3
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2',4'-Dihydroxyacetophenone (Standard)
0 ImagesSynonyms: Resacetophenone (Standard); 1-(2,4-Dihydroxyphenyl)ethanone (Standard)2',4'-Dihydroxyacetophenone (Resacetophenone) is acetophenone carrying hydroxy substituents at positions 2' and 4'. 2',4'-Dihydroxyacetophenone involves in a practical CsHCO3-mediated alkylation that efficiently provide 4-alkylated products with excellent regioselectivity, good isolated yields and a broad substrate scope. 2',4'-Dihydroxyacetophenone is a plant metabolite.
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COX-1/2-IN-6
0 ImagesCat. No.: HY-162044CAS No.: 327024-84-0
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7,4'-Dihydroxyflavone (Standard)
0 Images7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM.
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Phenyl β-D-glucopyranoside (Standard)
0 ImagesPhenyl β-D-glucopyranoside (Standard) is the analytical standard of Phenyl β-D-glucopyranoside (HY-W011849). This product is intended for research and analytical applications. Phenyl β-D-glucopyranoside is a component isolated from Phellodendron amurense, which has anti-inflammatory and anti-tumor 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 inhibits the expression of pro-inflammatory cytokines and related genes.
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Phenidone (Standard)
0 ImagesPhenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
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Indobufen (Standard)
0 ImagesSynonyms: Ibustrin (Standard)Indobufen (Standard) is the analytical standard of Indobufen. This product is intended for research and analytical applications. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
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NS-398 (Standard)
0 ImagesNS-398 (Standard) is the analytical standard of NS-398. This product is intended for research and analytical applications. NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
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Bromfenac sodium hydrate (Standard)
0 ImagesSynonyms: Bromfenac monosodium salt sesquihydrate (Standard)Bromfenac (sodium hydrate) (Standard) is the analytical standard of Bromfenac (sodium hydrate). This product is intended for research and analytical applications. Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium hydrate can be used in ocular inflammation research.
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Pectolinarigenin (Standard)
0 ImagesPectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
