cyclooxygenase

Esflurbiprofen is an inhibitor of COX-1 and COX-2.

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

Guaiacol (2-Methoxyphenol) is a precursor to various flavorants, such as eugenol and vanillin. Its derivatives are used medicinally as an expectorant, antiseptic, and local anesthetic. It also can be used as an indicator in chemical reactions that produce oxygen. When oxygen binds to it, the complex turns yellowish brown and absorbs light maximally at about 470 nm.

Ketorolac (Acuvail) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.

(±)-Catechin ((±)-Catechin hydrate) hydrate is a natural product,has antioxidant activity and is effective in reducing oxidative stress.

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Gallic acid (Benzoic acid) is found in almost all plants. Plants known for their high gallic acid content include gallnuts,grapes,tea,hops and oak bark.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Indomethacin (Indometacin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Lornoxicam (Chlortenoxicam) (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory, and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Lornoxicam is approved for use in Japan.

Revaprazan hydrochloride (YH1885) is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity.

Paradol ([6]-Gingerone) is a pungent phenolic substance found in ginger and other Zingiberaceae plants, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities,neuroprotective Effects.

Tenoxicam (Tilcotil), an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain.

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

2-Chloro-4-nitrophenol is a phenolic compound. It is an inhibitor of cyclooxygenase (COX), which reduces the production of prostaglandins, thereby reducing inflammation and pain.

CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin induces significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins. Nitroaspirin has antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.

Amtolmetin guacil (ST-679) inhibits prostaglandin synthesis and cyclooxygenase. Amtolmetin guacil has similar NSAID properties like tolmetin with additional analgesic, antipyretic, and gastroprotective properties.

4,7-DIHYDROXYCOUMARIN is a naturally occurring coumarin derivative found in a variety of plants, including parsley and chamomile. It has been found to inhibit the activity of several enzymes, including cytochrome P450, cyclooxygenase and lipoxygenase. It can also bind to DNA, regulate gene expression, and inhibit cell cycle progression. It can also induce apoptosis in tumor cells and reduce inflammation.

CGS 15435 is a potent thromboxen (TxA2) synthetase inhibitor (IC50: 1 nM). CGS 15435 acts on PGI2 synthase, cyclooxygenase and liposynthase with much less selectivity than on thromboxin synthase.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

Hamaline (9-(4-chlorobenzyl)-6-methoxy-1-methyl-4,9-dihydro-3H-pyrido[3,4-b]indole) is a substrate-selective cyclooxygenase-2 (COX-2) inhibitor.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

Butibufen (FF-106) is an orally active non-steroidal anti-inflammatory compound, a potential cyclooxygenase inhibitor with analgesic and antipyretic activity, and inhibits urea synthesis.Butibufen has been used in the study of rheumatic diseases.

Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 μM. Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively).

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins.

PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834

Catechin (Cianidanol) is a flavan-3-ol, a type of natural phenol and antioxidant.

Meloxicam (Metacam) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of meloxicam is as a Cyclooxygenase Inhibitor. The chemical classification of meloxicam is Nonsteroidal Anti-inflammatory Compounds.

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Etofenamate is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain.

Phenacetin (Acetophenetidin) is a phenylacetamide that was formerly used in ANALGESICS but nephropathy and METHEMOGLOBINEMIA led to its withdrawal from the market.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a COX-2 inhibitor wih anti-inflammatory activity.

Mefenamic acid (CN-35355) is a non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.

EIPA (L593754) (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Naproxen ((S)-Naproxen) is a propionic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities.

Deracoxib (SC 46) is a non-steroidal, non-narcotic anti-inflammatory drug. It is also a selective cyclooxygenase-2 inhibitor, and IC50 Value: 70 to 150 μM(inhibition of 3 osteosarcoma cell lines).

Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) suppressed the differentiation of naive CD4+ T cells into Th1 in vitro. Furthermore, Ethyl Caffeate intensely blocked the transcriptional expression in interferon-γ-related signaling, including IFN-γ, T-bet, STAT1, and STAT4.

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO)/cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg/ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg/ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.