COX-2 Selective Inhibitors

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
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 K_i of 0.06 μM. It also inhibits COX1 with K_i 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
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