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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Biguanide-4-(p-tolylethynyl)aniline
0 ImagesCat. No.: HY-189542CAS No.: 3112754-10-3Biguanide-4-(p-tolylethynyl) aniline is an amphiphilic cation and AMPK pathway phosphorylation inducer that crosses phospholipid membranes and accumulates in mitochondria, inhibiting pancreatic cancer cell proliferation by altering COXII and NDUFB8 protein levels. Biguanide-4-(p-tolylethynyl) aniline can be used in the study of pancreatic cancer.
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COX-2-IN-32
0 ImagesCat. No.: HY-153762CAS No.: 2725863-08-9COX-2-IN-32 (Compound 2f) is an iNOS and COX-2 inhibitor. COX-2-IN-32 decreases the expression of NF-κB. COX-2-IN-32 has anti-inflammatory activity by inhibits NO production in LPS-induced RAW264.7 macrophages (IC50: 11.2 μM).
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Loxoprofen sodium dihydrate
0 ImagesCat. No.: HY-B0578BCAS No.: 226721-96-6Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity.
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7-Methoxy-4H-chromen-4-one-o-carborane
0 ImagesCat. No.: HY-183188CAS No.: 3097646-97-1
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COX-1-IN-5
0 ImagesCat. No.: HY-160184CAS No.: 524699-85-2COX-1-IN-5 (example 13, compound PS13) is a potent and selective COX-1 inhibitor (COX-1 IC50 = 1 nM, COX-2 IC50 > 0.1 μM) exhibiting >1000-fold selectivity over COX-2. COX-1-IN-5 possesses strong anti-inflammatory, antipyretic, analgesic, antithrombotic, anti-cancer activities. COX-1-IN-5 can be used for COX-mediated diseases research, such as inflammatory conditions and pain. COX-1-IN-5 radiolabeled with 11C can be used as a selective PET tracer for whole‑body imaging of COX‑1 distribution and target engagement in vivo.
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COX-2-IN-19
0 ImagesCat. No.: HY-146198CAS No.: 2497530-12-6COX-2-IN-19 (Compound 24) is a potent COX-2 inhibitor with an IC50 of 1.76 μM. COX-2-IN-19 shows in vivo anti-inflammatory activity.
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COX-2-IN-52
0 ImagesCat. No.: HY-168888COX-2-IN-52 (Compound 5l) is an orally active and selective COX-2 inhibitor with an IC50 of 54 nM. COX-2-IN-52 can inhibit the release of NO in cells and has anti-inflammatory activity. COX-2-IN-52 has high gastrointestinal safety and can be used in the research of oral anti-inflammatory drugs.
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COX-2-IN-66
0 ImagesCat. No.: HY-183288COX-2-IN-66 is a cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 8.43 μM. COX-2-IN-66 reduces release of pro-inflammatory cytokines IL-6 and TNF-α. COX-2-IN-66 exhibits acceptable cellular tolerability, with cytokine-modulating concentrations remaining below its cytotoxic threshold. COX-2-IN-66 can be used for the research of inflammation.
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COX-2-IN-34
0 ImagesCOX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects.
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Antitumor agent-225
0 ImagesCat. No.: HY-187003CAS No.: 1338320-95-8Antitumor agent-225 is an orally effective and potent HDAC inhibitor with an IC50 value of 4.17 nM. Antitumor agent-225 inhibits HDAC activity by chelating zinc ions through its hydroxamic acid group, downregulates iNOS and COX-2 proteins, and suppresses the production of multiple inflammatory factors induced by LPS (HY-D1056). Antitumor agent-225 can be used for research on cancer and inflammation-related diseases.
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Santamarine
0 ImagesSantamarine (Santamarin; Balchanin) is a sesquiterpene lactone found in Artemisia scoparia. Santamarine shows anti-inflammatory, antioxidant, anticancer and anti-photoaging activities. Santamarine suppresses UVA-induced phosphorylation of JNK and p38 MAPK, nuclear translocation of phosphorylated c-Fos and c-Jun, and AP-1-mediated MMP-1 transcription and secretion. Santamarine suppresses NF-κB signaling, iNOS, COX-2, TNF-α, and IL-1β production. Santamarine inhibits thioredoxin reductase activity, induces ROS production, mitochondrial apoptosis, G2/M cell cycle arrest, and DNA damage, and reduces cancer cell growth. Santamarine can be used for the photoaging, inflammatory diseases and cancer.
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Myristinin A
0 ImagesCat. No.: HY-N16849CAS No.: 145904-69-4Synonyms: YM 26567-1Myristinin A (YM 26567-1) is a trans-isomer flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin A can selectively inhibit COX-2 activity with an IC50 of 16.9 μg/mL. Myristinin A can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin A can inhibit Candida albicans with an IC50 of 8.8 μg/mL. Myristinin A can be used for the research of inflammation and infection, such as rheumatoid arthritis.
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COX-2-IN-40
0 ImagesCat. No.: HY-162244CAS No.: 444790-64-1COX-2-IN-40 (compound 17) is a COX-2 inhibitor with the IC50 of 14.86 μM. COX-2-IN-40 can be used for study of chronic pain.
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COX-2-IN-29
0 ImagesCat. No.: HY-150721CAS No.: 3033545-21-7COX-2-IN-29 (Compound 15b) is a selective and orally active COX-2 inhibitor with an IC50 of 0.005 μM.
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Mefenamic acid-d4
0 ImagesMefenamic acid-d4 is a 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.
