COX-2
Cyclooxygenase-2 (COX-2) is an inducible enzyme catalyzing the conversion of arachidonic acid to prostaglandin endoperoxides, central to prostanoid biosynthesis and inflammatory signaling[1][2]. Mechanistically, COX-2 activity is regulated by both its catalytic and allosteric subunits, allowing modulation by fatty acids and selective inhibitors, distinguishing it from constitutive COX-1[2]. COX-2 is strongly upregulated in response to pro-inflammatory cytokines, hypoxia, and tumor microenvironment signals, orchestrating prostaglandin E2 (PGE2) production and downstream activation of NF-κB and PI3K-Akt pathways[3][4][5]. In disease models, COX-2 contributes to cancer progression, atherosclerosis, and migraine through modulation of immune responses, vascular smooth muscle activity, and neuronal-glial interactions[6][7][5]. Compared with COX-1, COX-2 expression is more context-dependent and spatially regulated, being highly inducible in endothelial cells, arterial versus venous smooth muscle, and neuronal populations under stress or inflammatory stimuli[8][9][10]. Experimental studies demonstrate COX-2 as a critical mediator of ischemic preconditioning in the heart, providing cardioprotection via PGE2 and PGI2 signaling[11]. Selective COX-2 inhibitors, including synthetic NSAIDs and dual COX/LOX modulators, are utilized to interrogate COX-2 function and develop anti-inflammatory therapies with reduced gastrointestinal and cardiovascular side effects[3][12]. Agonist studies further highlight receptor-mediated induction of COX-2, exemplifying its role in colon carcinoma and trigeminal ganglia models[13][7].
References:
- [1]. Smith FG, et al. Cyclooxygenase (COX) Inhibitors and the Newborn Kidney. Pharmaceuticals (Basel). 2012 Oct 25;5(11):1160-76. [Content Brief]
- [2]. Ahmadi M, et al. Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors. RSC Med Chem. 2022 Feb 14;13(5):471-496. [Content Brief]
- [3]. Bolli R, et al. Discovery of a new function of cyclooxygenase (COX)-2: COX-2 is a cardioprotective protein that alleviates ischemia/reperfusion injury and mediates the late phase of preconditioning. Cardiovasc Res. 2002 Aug 15;55(3):506-19. [Content Brief]
- [4]. Kirkby NS, et al. COX-2 protects against atherosclerosis independently of local vascular prostacyclin: identification of COX-2 associated pathways implicate Rgl1 and lymphocyte networks. PLoS One. 2014 Jun 2;9(6):e98165. [Content Brief]
- [5]. Segelcke D, et al. The role of the spinal cyclooxygenase (COX) for incisional pain in rats at different developmental stages. Eur J Pain. 2020 Feb;24(2):312-324. [Content Brief]
- [6]. Chatzipieris FP, et al. Recent advances in dual COX/LOX inhibitor design (2020-2024). Life. 2026;16(1):163. [Content Brief]
- [7]. Yang WL, et al. Cholinergic receptor up-regulates COX-2 expression and prostaglandin E(2) production in colon cancer cells. Carcinogenesis. 2000 Oct;21(10):1789-93. [Content Brief]
- [8]. Hsieh HL, et al. c-Src-dependent EGF receptor transactivation contributes to ET-1-induced COX-2 expression in brain microvascular endothelial cells. J Neuroinflammation. 2012 Jul 2;9:152. [Content Brief]
- [9]. Neeb L, et al. IL-1β stimulates COX-2 dependent PGE₂ synthesis and CGRP release in rat trigeminal ganglia cells. PLoS One. 2011 Mar 4;6(3):e17360. [Content Brief]
- [10]. Chen S, et al. 288 The COX-2 pathway as a mediator of resistance to anti-PD-1 therapy. J Immunother Cancer. 2021;9(Suppl 2):A312.
- [11]. Bishop-Bailey D, et al. Differential induction of cyclooxygenase-2 in human arterial and venous smooth muscle: role of endogenous prostanoids. Arterioscler Thromb Vasc Biol. 1998 Oct;18(10):1655-61. [Content Brief]
- [12]. Majumder M, et al. COX-2 Elevates Oncogenic miR-526b in Breast Cancer by EP4 Activation. Mol Cancer Res. 2015 Jun;13(6):1022-33. [Content Brief]
- [13]. Scott KF, et al. Functional coupling and differential regulation of the phospholipase A2-cyclooxygenase pathways in inflammation. J Leukoc Biol. 1999 Oct;66(4):535-41. [Content Brief]
- [14]. Smith WL, et al. Interactions of fatty acids, nonsteroidal anti-inflammatory drugs, and coxibs with the catalytic and allosteric subunits of cyclooxygenases-1 and -2. J Biol Chem. 2019 Feb 1;294(5):1697-1705. [Content Brief]
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COX-2 Related Products (516)
Related Products (516)
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Ketorolac tromethamine salt
0 ImagesSynonyms: Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt
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Humulone
0 ImagesSynonyms: α-Lupulic acidHumulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
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Glafenine hydrochloride
0 ImagesSynonyms: Glafenin hydrochlorideGlafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF).
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Dendrophenol
0 ImagesSynonyms: MoscatilinDendrophenol (Moscatilin) is a NF-κB inhibitor that inhibits inflammation. Dendrophenol exerts potent cytotoxic effect against tumor cells and induces cell cycle arrest and apoptosis. Dendrophenol has antitumor activity. In addition, Dendrophenol can inhibit vascular calcification by inhibiting the activation of WNT3/β-catenin.
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Lornoxicam
0 ImagesSynonyms: Chlortenoxicam; Ro 13-9297Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer.
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Geranial
0 ImagesSynonyms: (E)-3,7-Dimethylocta-2,6-dienalGeranial is an aromatic compound. It can be isolated from the fruits of Litsea cubeba Lour and the rhizomes of ginger (Zingiber officinale). Geranial inhibits LPS-induced phosphorylation of ERK1/2, JNK1/3 and IκB in macrophages. It suppresses the secretion of IL-1β, TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2. Geranial increases ROS. It can be used in the research of inflammatory diseases.
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Pranoprofen
0 ImagesPranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.
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Ecliptasaponin A
0 ImagesEcliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.
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[10]-Shogaol
![[10]-Shogaol](https://file.medchemexpress.com/product_pic/hy-n2434.gif "Click to View [10]-Shogaol Product Detail")
0 Images[10]-Shogaol is an orally active antioxidant. [10]-Shogaol can be extracted from ginger (Zingiber officinale). [10]-Shogaol1 inhibits COX-2 with an IC50 value of 7.5 μM. [10]-Shogaol inhibits the production of proinflammatory cytokines (IL-1β, IL-6). [10]-Shogaol inhibits NF-κB phosphorylation. [10]-Shogaol has anti-inflammatory effects. [10]-Shogaol has anticancer effects against Docetaxel (HY-B0011)-resistant prostate cancer. [10]-Shogaol exhibits larvicidal activity against L5 larvae of Angiostrongylus cantonensis.
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Hexahydrocurcumin
0 ImagesHexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities.
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DuP-697
0 ImagesDuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
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Octahydrocurcumin
0 ImagesSynonyms: HexahydrobisdemethoxycurcuminOctahydrocurcumin (Hexahydrobisdemethoxycurcumin) is an orally active anticancer and anti-inflammatory agent, and is the final hydrogenated metabolite of Curcumin (HY-N0005) in vivo. Octahydrocurcumin exerts its anti-tumor and anti-inflammatory effects by inducing the mitochondrial apoptosis pathway and inhibiting the TAK1-NF-κB-COX-2 pathway, respectively.
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Anthraquinone-2-carboxylic acid
0 ImagesAnthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n
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FK 3311
0 ImagesSynonyms: COX-2 Inhibitor VFK 3311 (COX-2 Inhibitor V) is a selective inhibitor of COX-2 with antiinflammatory agent.
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Tenoxicam
0 ImagesSynonyms: Ro-12-0068Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
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Loxoprofen
0 ImagesLoxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity.
