COX
Cyclooxygenase
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
All Product Categories
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COX Related Products (1325)
Related Products (1325)
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Antibodies (6)
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COX Isoform Comparison
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Hydralazine-d5 (hydrochloride)
0 ImagesHydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.
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Polmacoxib
0 ImagesSynonyms: CG100649Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models.
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Hordenine-d6
0 ImagesSynonyms: Ordenina-d6; Peyocactine-d6Hordenine-d6 (Ordenina-d6; Peyocactine-d6) is the deuterated-labeled Hordenine (HY-N0113). Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
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Celecoxib-d7
0 ImagesSynonyms: SC 58635-d7Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
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Nabumetone-d3
0 ImagesSynonyms: BRL14777-d3Nabumetone-d3 is the deuterium labeled Nabumetone (HY-B0559). Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metaboliteα-Demethylnaproxen (HY-W086896). Nabumetone can inhibit cancer cells proliferation and relieve gastric ulcers.
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Ibuprofen-d3 sodium
0 ImagesSynonyms: (±)-Ibuprofen-d3 sodiumIbuprofen-d3 ((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.
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(R)-Ketoprofen
0 ImagesCat. No.: HY-W322573CAS No.: 56105-81-8(R)-Ketoprofen is an orally active nonsteroidal anti-inflammatory drug (NSAID) with analgesic properties. (R)-Ketoprofen does not significantly amplify the increase of inflammatory cytokines (such as tumor necrosis factor (TNF) and interleukin-1 (IL-1)) induced by LPS, but it can inhibit the anti-inflammatory activity of (S)-Ketoprofen.
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Phellodendrine
0 ImagesPhellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
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Acetaminophen-d3
0 ImagesSynonyms: Paracetamol-d3; 4-Acetamidophenol-d3; 4'-Hydroxyacetanilide-d3Acetaminophen-d3 is the deuterium 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.
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Desoxo-narchinol A
0 ImagesDesoxo-narchinol A is an orally active and potent anti-inflammatory agent. Desoxo-narchinol A can be isolated from the roots and rhizomes of Nardostachys jatamansi. Desoxo-narchinol A can be used for septic shock and inflammatory diseases research.
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Flufenamic acid-13C6
0 ImagesCat. No.: HY-B1221S1CAS No.: 1325559-30-5Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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Celecoxib-d3
0 ImagesSynonyms: SC 58635-d3Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
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APHS
0 ImagesAPHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition.
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Diclofenac-13C6
0 ImagesDiclofenac-13C6 is the 13C6 labeled Diclofenac. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
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(-)-Epiafzelechin
0 Images(−)-Epiafzelechin is a COX-1 inhibitor with an IC50 of approximately 15 μM against COX-1 activity. (−)-Epiafzelechin also exhibits DPPH free radical scavenging activity, with an EC50 of 20.9 μM. (−)-Epiafzelechin promotes osteoblast differentiation by increasing ALP activity, ECM collagen content and Runx2 expression, while reducing the growth of osteoclast precursors and RANKL-induced TRAP activity, thereby regulating the bone remodeling process. (−)-Epiafzelechin alleviates ovariectomy-induced bone loss. (−)-Epiafzelechin can be used in studies related to bone remodeling, postmenopausal osteoporosis, inflammatory responses and oxidative stress.
