COX

(-)-Catechin ((-)-Cianidanol), an isomer of catechin, inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.

Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG

(-)-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.

Ginsenoside C-K (Ginsenoside K) is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.

Emapalumab (NI-0501) is an IgG1 monoclonal antibody that humanizes human monoclonal antibodies against interferon gamma, blocking its binding to cell surface receptors and activating inflammatory signaling. Emapalumab has a high binding force (Kd=1.4 pM) to free IFN-γ and to IFN-γ bound to its receptor. Emapalumab can be used in the study of hemophagocytic lymphohistiocytosis (HLH).

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

Micheliolide(MCL) is a sesquiterpene lactone which inhibits various inflammatory response.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Celecoxib (SC 58635) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of celecoxib is as a Cyclooxygenase Inhibitor.

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.

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.

Xanthohumol, also known as 2', 4, 4'-trihydroxy-6'-methoxy-3'-prenylchalcone or desmethylxanthohumol, is a member of the class of compounds known as 3-prenylated chalcones. It inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

Benoxaprofen (NSC-299582) is a non-steroidal anti-inflammatory drug.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK ATM Chk1 2 pathway, leading to inactivation of the Cd

DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values ​​of 10 nM and 800 nM for human COX-2 and COX-1. DuP-697 also exhibits anti-angiogenic, anti-inflammatory, antipyretic and apoptotic effects.

Chebulagic acid, isolated from the Terminalia chebula Retz, is a COX-LOX dual inhibitor.

Prim-O-glucosylcimifugin (Cimifugin 7-glucoside) can inhibit the proliferation of SMC(smooth muscle cell) stimulated by TNF-alpha, increase the proportion of G0 G1 phase.

Quercimeritrin (Quercetin-7-O-beta-D-glucopyranoside) has antibacterial activity, it shows promising activity against Staphylococcus aureus.

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.

Sulfasalazine (Azulfidine) is a synthetic salicylic acid derivative with affinity for elastin-containing connective tissues and formulated as a prodrug. Sulfasalazine induces iron death and inhibits NF-κB, TGF-β and COX-2.

Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5 210 μg mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.

BN-82451 2HCl is a dual inhibitor of COX-1 and COX-2 and can be used to study Huntington's chorea and Parkinson's disease.

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

1. Pectolinarigenin (Pectolinaringenin) exhibits hepatoprotective activity mainly via SOD antioxidant mechanism. 2. Pectolinarigenin possesses anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions.

Indomethacin sodium hydrate (Indometacin sodium hydrate) is an orally active, competitive and reversible COX1 2 inhibitor with potential anti-inflammatory activity in induced migraines, induced gastrointestinal injuries, and may be used in studies of increased intracranial pressure secondary to severe traumatic brain injury and rheumatoid arthritis in adults.

SC-75416 is a selective COX-2 inhibitor for the study of pain.

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis 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.

β-Elemonic Acid (3-Oxotirucallenoic Acid) exhibits anti-inflammatory effects. Beta-Elemonic acid inhibits proliferation by inducing hypoploid cells and cell apoptosis, the anticancer effects of beta-Elemonic acid are related to the MAPK signaling pathway, ROS activation and glutathione depletion in human A549 lung cancer cells. Beta-Elemonic acid exhibits prolyl endopeptidase inhibitory activities.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

Paeoniflorin (Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall.

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

(-)-Catechin gallate ((-)-Catechin 3-O-gallate) displays inhibition of 6PGD, IDH. (-)-Catechin gallate ((-)-Catechin 3-O-gallate) displays inhibition of human Beta-secretase. (-)-Catechin gallate ((-)-Catechin 3-O-gallate) possesses antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 and chloroquine-resistant Plasmodium falciparum K1.

α-Humulene (Alpha-caryophyllene) is extracted from S.officinalis essential oil.α-Humulene can inhibit tumor cell growth.α-Humulene also shows anti-inflammatory effects, probably by interfering with TNFalpha production and COX-2 and iNOS expression.

[8]-Shogaol is a component of ginger and maintains anti-inflammatory activity as a cyclooxygenase-2 inhibitor.

Hexahydrocurcumin is a selective, orally active COX-2 inhibitor and inactive against COX-1.

Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM).

Isoorientin (Homoorientin) has antioxidant activity.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

Indomethacin (Indomethacin) is a COX1 and COX2 inhibitor (IC50=18 26 nM) with blood-brain barrier permeability and non-selectivity. Indomethacin is a non-steroidal anti-inflammatory agent with anti-tumor and anti-infective activity.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.

Eltenac (B78820) is a non-steroidal anti-inflammatory, COX inhibitor with analgesic activity.Eltenac inhibits COX-1 and COX-2 and is used in the study of Acute Respiratory Distress Syndrome (ARDS).

1. Gamabufotalin (Gamabufagin) , a major bufadienolide of Chansu, has been used for treatment of COX-2-mediated diseases and cancer therapy due to its desirable metabolic stability and less adverse effect.

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Ibuprofen Lysine (Neoprofen) is a non-steroidal anti-inflammatory drug.

Minoxidil (U10858) is an orally administered vasodilator with hair growth stimulatory and antihypertensive effects.

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