S0761 |
Desmethyl Celecoxib |
Desmethyl Celecoxib (compound 3b), an analog of Celecoxib with the optimal yield of 75%, is a selective inhibitor of cyclooxygenase-2 (COX-2) with anti-inflammatory activities. |
Selective |
|
S5711 |
Deracoxib |
Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). |
Selective |
|
S3283 |
Marmesin |
Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. |
Selective |
|
S4656 |
Parecoxib |
Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor. |
Selective |
|
S2349 |
Rutaecarpine |
Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor. |
Selective |
|
S9190 |
Oroxin B |
Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer. |
Selective |
|
S6685 |
Mavacoxib |
Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). |
Selective |
|
S2995 |
4-Hydroxyphenylpyruvic acid |
4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development. |
Selective |
|
S3255 |
Pectolinarigenin |
Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). |
Selective |
|
S4049 |
Valdecoxib |
Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM. |
Selective |
COX-2, IC50: 5 nM |
S0762 |
SC 236 |
SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity. |
Selective |
COX-2, IC50: 10 nM |
S3043 |
Rofecoxib |
Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM. |
Selective |
COX-2, IC50: 18 nM |
S4136 |
Carprofen |
Carprofen inhibits canine COX2 with IC50 of 30 nM. |
Selective |
canine COX2, IC50: 30 nM |
S1261 |
Celecoxib |
Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
Selective |
COX-2, IC50: 40 nM |
S2903 |
Lumiracoxib |
Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM. |
Selective |
COX-2, Ki: 60 nM |
S1959 |
Tolfenamic Acid |
Tolfenamic Acid(Clotam) is a COX-2 inhibitor with IC50 of 0.2 μM. |
Selective |
COX-2, IC50: 0.2 μM |
s8433 |
NS-398 (NS398) |
NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively. |
Selective |
COX-2, IC50: 3.8 μM |
S2040 |
Nimesulide |
Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM. |
Selective |
COX-2, IC50: 26 μM |
S3018 |
Niflumic acid |
Niflumic acid(Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain. |
Selective |
|
S3899 |
Hederagenin |
Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. |
Selective |
|
S3261 |
Myrislignan |
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation. |
Selective |
|
S3872 |
Guaiacol |
Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. |
Selective |
|
S3304 |
Stylopine |
Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L. |
Selective |
|
S9502 |
Madecassic acid |
Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition. |
Selective |
|
S4651 |
Etoricoxib |
Etoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia) is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties. |
Selective |
|
S5595 |
3-Carene |
3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. |
Selective |
|
S1576 |
Sulfasalazine |
Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. |
Selective |
|
S3931 |
Ginsenoside Rd |
Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP |
Selective |
|
S9208 |
Ginsenoside Rb3 |
Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also |
Selective |
|
S6850 |
NE 52-QQ57 |
NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric |
Selective |
|
S2595 |
FK-3311 |
FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. |
Selective |
|
S2531 |
Asaraldehyde |
Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1. |
Selective |
|
S4028 |
Dexamethasone Sodium Phosphate |
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
Selective |
|
S3816 |
Dehydroevodiamine |
Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. |
Selective |
|
S0931 |
Jaceosidin |
Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. |
Selective |
|
S2047 |
Lornoxicam |
Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis. |
Pan |
COX-2, IC50: 8 nM |
S5698 |
Ketorolac tromethamine salt |
Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. |
Pan |
COX2, IC50: 20 nM |
S5192 |
S-(+)-Ketoprofen |
S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively. |
Pan |
COX-2, IC50: 27 nM |
S4295 |
Meclofenamate Sodium |
Meclofenamate Sodium(CI 583) is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor. |
Pan |
COX-2, IC50: 50 nM |
S4149 |
Amfenac Sodium Monohydrate |
Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively. |
Pan |
COX-2, IC50: 150 nM |
S1903 |
Diclofenac Sodium |
Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. |
Pan |
COX-2, IC50: 200 nM |
S5010 |
Indometacin Sodium |
Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. |
Pan |
COX2, IC50: 0.78 μM |
S1396 |
Resveratrol |
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
Pan |
COX2, IC50: 1.3 μM |
S1646 |
Ketorolac |
Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. |
Pan |
COX-2 (human), IC50: 3.50 μM |
S1626 |
Naproxen Sodium |
Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. |
Pan |
COX-2, IC50: 5.2 μM |
S6686 |
SC-560 |
SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. |
Pan |
COX-2, IC50: 6.3 μM |
S1723 |
Indomethacin |
Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling. |
Pan |
COX-2, IC50: 14 μM |
S1634 |
Acetaminophen |
Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively. |
Pan |
COX2, IC50: 25.8 μM |
S1638 |
Ibuprofen (NSC 256857) |
Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. |
Pan |
COX-2, IC50: 370 μM |
S1255 |
Nepafenac |
Nepafenac (AHR 9434, AL 6515) is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery. |
Pan |
|
S2351 |
Salicin |
Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor. |
Pan |
|
S1645 |
Ketoprofen |
Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. |
Pan |
|
S4078 |
Mefenamic Acid |
Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2. |
Pan |
|
s7889 |
Xanthohumol |
Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. |
Pan |
|
S3008 |
Zaltoprofen |
Zaltoprofen(CN100,Soleton) is an inhibitor of COX-1 and COX-2 for treatment of arthritis. |
Pan |
|
S3017 |
Aspirin (NSC 27223) |
Aspirin (NSC 27223, Acetylsalicylic acid, ASA) is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy. |
Pan |
|
S1761 |
Suprofen |
Suprofen(TN-762) is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic. |
Pan |
|
S4230 |
Oxaprozin |
Oxaprozin (WY-21743,nsc 310839) is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis. |
Pan |
|
S4248 |
Bromfenac Sodium |
Bromfenac Sodium (AHR 10282R,Bromsite,Bromday,Prolensa,Xibrom) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. |
Pan |
|