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Catalog No. Product Name Information Product Use Citations Product Validations
E0226New Chebulagic acid

Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
E0500New Firocoxib (ML 1785713) Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood.
S0759 FPL 62064 FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity.
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.
S0766 RHC 80267 RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).
S0821 Pamicogrel Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties.
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.
S1204 Melatonin (NSC 113928) Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
Int J Mol Sci, 2021, 22(11)5649
Int Immunopharmacol, 2021, 96:107787
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.
Adv Sci (Weinh), 2020, 7(21):2001018
S1261 Celecoxib (SC 58635) Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
Nat Commun, 2022, 13(1):1487
Hypertens Res, 2022, 10.1038/s41440-022-00889-1
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1328 Etodolac Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.
Genome Med, 2021, 13(1):168
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-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.
Placenta, 2022, 122:56-65
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
S1518 Ibuprofen Lysine Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 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.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
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.
Drug Metab Dispos, 2020, 48(8):613-621
Adv Ther (Weinh), 2020, 2000034
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.
Immunity, 2020, 52(2):328-341
Anticancer Drugs, 2020, 31(1):27-34
Virol Sin, 2019, 34(6):648-661
S1645 Ketoprofen Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.
Signal Transduct Target Ther, 2022, 7(1):46
J Nucl Med, 2020, jnumed.120.249367
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.
J Virol, 2020, 6;94(2):e01679-19
Life Sci, 2020, 15;251:117604
S1713 Piroxicam Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.
S1723 Indomethacin (NSC-77541) Indomethacin (NSC-77541, Indometacin) 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.
J Exp Clin Cancer Res, 2021, 40(1):344
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00738-w
Front Endocrinol (Lausanne), 2021, 12:665145
S1734 Meloxicam Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.
J Oncol, 2022, 2022:4598573
PLoS One, 2020, 13;15(3):e0230272
Oncol Lett, 2017, 14(2):2198-2206
S1761 Suprofen Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
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.
Oxid Med Cell Longev, 2018, 2018:3692752
Arch Toxicol, 2018, 92(6):1953-1967
Cell, 2016, 167(7):1803-1813
S1959 Tolfenamic Acid Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM.
Hum Mol Genet, 2020, ddaa244
Front Microbiol, 2020, 10:2936
Oncotarget, 2017, 8(57):96865-96884
S1960 Pranoprofen Pranoprofen (Pyranoprofen) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
Front Immunol, 2020, 11:534099
Mol Med Rep, 2017, 15(6):4305-4311
S2007 Sulindac Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2040 Nimesulide Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.
Front Microbiol, 2020, 10:2936
Elife, 2016, 5e14653
Viruses, 2015, 7(5):2268-87
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.
S2108 Flunixin Meglumin Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.
S2121 Licofelone (ML3000) Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis.
Hum Mol Genet, 2020, ddaa244
S2272 Indoprofen Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein.
S2349 Rutaecarpine Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor.
Theranostics, 2020, 10(8):3366-3381
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.
Biochem Biophys Res Commun, 2019, 508(3):682-689
S2410 Paeoniflorin (NSC 178886) Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2531 Asaraldehyde Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
S2577 Phenacetin Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties.
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.
S2602 Acemetacin Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
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.
Int J Biol Macromol, 2021, 187:603-613
Cells, 2020, 9(9)E2005
J Am Heart Assoc, 2020, 9(1):e013470
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.
S3008 Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Dev Cell, 2021, S1534-5807(21)00485-8
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021
S3018 Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S3023 Bufexamac Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.
Int J Mol Sci, 2021, 22(9)4559
Reprod Sci, 2021, 10.1007/s43032-021-00533-2
Autophagy, 2016, 12(10):1738-1758
S3043 Rofecoxib Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM.
Toxicol Appl Pharmacol, 2015, 285(1):51-60
S3063 Diclofenac Diethylamine Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency.
S3168 cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S3173 Antipyrine Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor.
S3200 Triflusal Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.
J Am Heart Assoc, 2020, 9(1):e013470
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).
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.
S3283 Marmesin Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity.
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.
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.
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.
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.
S3925 (-)-Epicatechin gallate (-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM.
Cell Death Dis, 2018, 9(2):205
PLoS One, 2018, 13(10):e0205123
J Fish Dis, 2018, 10.1111/jfd.12819
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, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3969 Veratric acid Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
S3974 (+)-Catechin hydrate Catechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
J Steroid Biochem Mol Biol, 2021, 211:105906
S4011 Ampiroxicam Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
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.
Pharmaceutics, 2022, 14(2)400
Dis Model Mech, 2022, dmm.049109
Hematology, 2022, 27(1):32-42
S4032 Bismuth Subsalicylate Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
S4049 Valdecoxib Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(10):110490
Biochem Bioph Res Co, 2015, 460(2):198-204
S4051 Nabumetone Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
S4078 Mefenamic Acid Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2.
Am J Physiol Renal Physiol, 2022, 10.1152/ajprenal.00568.2020
Brain Res, 2020, 20;1740:146846
S4136 Carprofen Carprofen inhibits canine COX2 with IC50 of 30 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.
S4176 Trometamol Trometamol is a proton acceptor used to treat acidemia. It inhibits both isoforms of cyclooxygenases (COX1 and COX2), thereby blocking the conversion of arachidonic acid to pro-inflammatory pro-prostaglandins.
S4230 Oxaprozin Oxaprozin (WY-21743) 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.
S4248 Bromfenac Sodium Bromfenac Sodium (AHR 10282R) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.
S4295 Meclofenamate Sodium Meclofenamate Sodium 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.
Front Oncol, 2022, 12:817584
Nature, 2019, 573(7775):539-545
S4360 Tolmetin Sodium Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor.
S4435 Metamizole sodium hydrate Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties.
S4509 4-Aminoantipyrine 4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols.
S4526 Fenbufen Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.
Gastroenterology, 2019, 10.1053/j
S4539 Salicylic acid Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
S4609 Diflunisal Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget) is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor.
S4628 (+/-)-Sulfinpyrazone Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
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.
Virol Sin, 2019, 34(6):648-661
S4656 Parecoxib Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor.
Theranostics, 2020, 10(8):3366-3381
S4686 Vitamin E Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
Bone Res, 2022, 10(1):26
EMBO Mol Med, 2022, 14(2):e14903
Biosci Biotechnol Biochem, 2020, 18;1-8
S4765 Syringaldehyde Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities.
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.
J Exp Clin Cancer Res, 2021, 40(1):344
Mol Cell, 2020, 80(3):525-540.e9
Mol Cancer Ther, 2020, 19;molcanther00152020
S5019 Indobufen Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis.
S5177 Naproxen Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2.
Drug Metab Dispos, 2020, 48(8):613-621
Biogerontology, 2016, 17(5-6):907-920
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.
S5309 Propyphenazone (4-Isopropylantipyrine) Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity.
S5418 Parecoxib Sodium Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2).
S5520 Phenidone Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer.
S5551 6-Paradol 6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2.
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.
Phytomedicine, 2021, 91:153707
S5640 Ethyl caffeate Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro.
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.
Front Immunol, 2021, 12:616402
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).
S5786 Bromfenac sodium hydrate Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively.
S6073 Diclofenac acid Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency.
S6457 Flurbiprofen Axetil Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase.
S6615 ATB 346 ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells.
S6685 Mavacoxib Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID).
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.
S6780 TFAP TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM.
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 oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
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.
Oxid Med Cell Longev, 2022, 2022:9523491
Int J Mol Sci, 2021, 22(22)12134
J-Cancer, 2020, 6;11-14-:4047-4058
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.
PLoS Negl Trop Dis, 2022, 16(4):e0010402
Mol Oncol, 2021, 10.1002/1878-0261.13077
Oxid Med Cell Longev, 2021, 2021:7394344
S9029 Prim-o-glucosylcimifugin Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner.
S9149 Benzoylpaeoniflorin Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro.
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.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment.
Theranostics, 2022, 12(2):910-928
J Cancer, 2021, 12(7):2140-2150
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 inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).
S9236 α-Cyperone α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1.
S9386 Polygalacic acid Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner.
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.
E0226New Chebulagic acid

Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
E0500New Firocoxib (ML 1785713) Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood.
S0759 FPL 62064 FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity.
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.
S0766 RHC 80267 RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).
S0821 Pamicogrel Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties.
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.
S1204 Melatonin (NSC 113928) Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
Int J Mol Sci, 2021, 22(11)5649
Int Immunopharmacol, 2021, 96:107787
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.
Adv Sci (Weinh), 2020, 7(21):2001018
S1261 Celecoxib (SC 58635) Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
Nat Commun, 2022, 13(1):1487
Hypertens Res, 2022, 10.1038/s41440-022-00889-1
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1328 Etodolac Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.
Genome Med, 2021, 13(1):168
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-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.
Placenta, 2022, 122:56-65
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
S1518 Ibuprofen Lysine Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 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.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
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.
Drug Metab Dispos, 2020, 48(8):613-621
Adv Ther (Weinh), 2020, 2000034
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.
Immunity, 2020, 52(2):328-341
Anticancer Drugs, 2020, 31(1):27-34
Virol Sin, 2019, 34(6):648-661
S1645 Ketoprofen Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.
Signal Transduct Target Ther, 2022, 7(1):46
J Nucl Med, 2020, jnumed.120.249367
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.
J Virol, 2020, 6;94(2):e01679-19
Life Sci, 2020, 15;251:117604
S1713 Piroxicam Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.
S1723 Indomethacin (NSC-77541) Indomethacin (NSC-77541, Indometacin) 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.
J Exp Clin Cancer Res, 2021, 40(1):344
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00738-w
Front Endocrinol (Lausanne), 2021, 12:665145
S1734 Meloxicam Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.
J Oncol, 2022, 2022:4598573
PLoS One, 2020, 13;15(3):e0230272
Oncol Lett, 2017, 14(2):2198-2206
S1761 Suprofen Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
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.
Oxid Med Cell Longev, 2018, 2018:3692752
Arch Toxicol, 2018, 92(6):1953-1967
Cell, 2016, 167(7):1803-1813
S1959 Tolfenamic Acid Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM.
Hum Mol Genet, 2020, ddaa244
Front Microbiol, 2020, 10:2936
Oncotarget, 2017, 8(57):96865-96884
S1960 Pranoprofen Pranoprofen (Pyranoprofen) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
Front Immunol, 2020, 11:534099
Mol Med Rep, 2017, 15(6):4305-4311
S2007 Sulindac Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2040 Nimesulide Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.
Front Microbiol, 2020, 10:2936
Elife, 2016, 5e14653
Viruses, 2015, 7(5):2268-87
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.
S2108 Flunixin Meglumin Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.
S2121 Licofelone (ML3000) Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis.
Hum Mol Genet, 2020, ddaa244
S2272 Indoprofen Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein.
S2349 Rutaecarpine Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor.
Theranostics, 2020, 10(8):3366-3381
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.
Biochem Biophys Res Commun, 2019, 508(3):682-689
S2410 Paeoniflorin (NSC 178886) Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2531 Asaraldehyde Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
S2577 Phenacetin Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties.
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.
S2602 Acemetacin Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
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.
Int J Biol Macromol, 2021, 187:603-613
Cells, 2020, 9(9)E2005
J Am Heart Assoc, 2020, 9(1):e013470
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.
S3008 Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Dev Cell, 2021, S1534-5807(21)00485-8
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021
S3018 Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S3023 Bufexamac Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.
Int J Mol Sci, 2021, 22(9)4559
Reprod Sci, 2021, 10.1007/s43032-021-00533-2
Autophagy, 2016, 12(10):1738-1758
S3043 Rofecoxib Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM.
Toxicol Appl Pharmacol, 2015, 285(1):51-60
S3063 Diclofenac Diethylamine Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency.
S3168 cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S3173 Antipyrine Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor.
S3200 Triflusal Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.
J Am Heart Assoc, 2020, 9(1):e013470
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).
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.
S3283 Marmesin Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity.
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.
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.
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.
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.
S3925 (-)-Epicatechin gallate (-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM.
Cell Death Dis, 2018, 9(2):205
PLoS One, 2018, 13(10):e0205123
J Fish Dis, 2018, 10.1111/jfd.12819
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, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3969 Veratric acid Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
S3974 (+)-Catechin hydrate Catechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
J Steroid Biochem Mol Biol, 2021, 211:105906
S4011 Ampiroxicam Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
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.
Pharmaceutics, 2022, 14(2)400
Dis Model Mech, 2022, dmm.049109
Hematology, 2022, 27(1):32-42
S4032 Bismuth Subsalicylate Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
S4049 Valdecoxib Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(10):110490
Biochem Bioph Res Co, 2015, 460(2):198-204
S4051 Nabumetone Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
S4078 Mefenamic Acid Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2.
Am J Physiol Renal Physiol, 2022, 10.1152/ajprenal.00568.2020
Brain Res, 2020, 20;1740:146846
S4136 Carprofen Carprofen inhibits canine COX2 with IC50 of 30 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.
S4176 Trometamol Trometamol is a proton acceptor used to treat acidemia. It inhibits both isoforms of cyclooxygenases (COX1 and COX2), thereby blocking the conversion of arachidonic acid to pro-inflammatory pro-prostaglandins.
S4230 Oxaprozin Oxaprozin (WY-21743) 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.
S4248 Bromfenac Sodium Bromfenac Sodium (AHR 10282R) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.
S4295 Meclofenamate Sodium Meclofenamate Sodium 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.
Front Oncol, 2022, 12:817584
Nature, 2019, 573(7775):539-545
S4360 Tolmetin Sodium Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor.
S4435 Metamizole sodium hydrate Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties.
S4509 4-Aminoantipyrine 4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols.
S4526 Fenbufen Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.
Gastroenterology, 2019, 10.1053/j
S4539 Salicylic acid Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
S4609 Diflunisal Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget) is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor.
S4628 (+/-)-Sulfinpyrazone Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
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.
Virol Sin, 2019, 34(6):648-661
S4656 Parecoxib Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor.
Theranostics, 2020, 10(8):3366-3381
S4686 Vitamin E Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
Bone Res, 2022, 10(1):26
EMBO Mol Med, 2022, 14(2):e14903
Biosci Biotechnol Biochem, 2020, 18;1-8
S4765 Syringaldehyde Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities.
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.
J Exp Clin Cancer Res, 2021, 40(1):344
Mol Cell, 2020, 80(3):525-540.e9
Mol Cancer Ther, 2020, 19;molcanther00152020
S5019 Indobufen Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis.
S5177 Naproxen Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2.
Drug Metab Dispos, 2020, 48(8):613-621
Biogerontology, 2016, 17(5-6):907-920
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.
S5309 Propyphenazone (4-Isopropylantipyrine) Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity.
S5418 Parecoxib Sodium Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2).
S5520 Phenidone Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer.
S5551 6-Paradol 6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2.
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.
Phytomedicine, 2021, 91:153707
S5640 Ethyl caffeate Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro.
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.
Front Immunol, 2021, 12:616402
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).
S5786 Bromfenac sodium hydrate Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively.
S6073 Diclofenac acid Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency.
S6457 Flurbiprofen Axetil Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase.
S6615 ATB 346 ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells.
S6685 Mavacoxib Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID).
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.
S6780 TFAP TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM.
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 oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
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.
Oxid Med Cell Longev, 2022, 2022:9523491
Int J Mol Sci, 2021, 22(22)12134
J-Cancer, 2020, 6;11-14-:4047-4058
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.
PLoS Negl Trop Dis, 2022, 16(4):e0010402
Mol Oncol, 2021, 10.1002/1878-0261.13077
Oxid Med Cell Longev, 2021, 2021:7394344
S9029 Prim-o-glucosylcimifugin Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner.
S9149 Benzoylpaeoniflorin Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro.
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.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment.
Theranostics, 2022, 12(2):910-928
J Cancer, 2021, 12(7):2140-2150
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 inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).
S9236 α-Cyperone α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1.
S9386 Polygalacic acid Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner.
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.
E0226New Chebulagic acid

Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
E0500New Firocoxib (ML 1785713) Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood.
Tags: COX inhibitor|COX agonist|COX activator|COX inducer|COX antagonist|COX signaling pathway|COX assay kit