COX

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1261	Celecoxib (SC 58635)	<1 mg/mL	76 mg/mL	'33 mg/mL
S1396	Resveratrol (SRT501)	<1 mg/mL	45 mg/mL	''<1 mg/mL
S1255	Nepafenac	<1 mg/mL	50 mg/mL	<1 mg/mL
S1638	Ibuprofen (NSC 256857)	<1 mg/mL	41 mg/mL	'41 mg/mL
S1723	Indomethacin (NSC-77541)	<1 mg/mL	72 mg/mL	''24 mg/mL
S5786	Bromfenac sodium hydrate	100 mg/mL	100 mg/mL	''<1 mg/mL
S4435	Metamizole sodium hydrate	70 mg/mL	70 mg/mL	''35 mg/mL
S5192	S-(+)-Ketoprofen	<1 mg/mL	51 mg/mL	''51 mg/mL
S2007	Sulindac	<1 mg/mL	71 mg/mL	9 mg/mL
S3043	Rofecoxib	<1 mg/mL	63 mg/mL	<1 mg/mL
S1734	Meloxicam	<1 mg/mL	30 mg/mL	<1 mg/mL
S4028	Dexamethasone Sodium Phosphate	103 mg/mL	<1 mg/mL	''<1 mg/mL
S3023	Bufexamac	<1 mg/mL	45 mg/mL	'3 mg/mL
S1204	Melatonin (NSC 113928)	<1 mg/mL	47 mg/mL	''47 mg/mL
S3017	Aspirin (NSC 27223)	<1 mg/mL	36 mg/mL	''36 mg/mL
S1761	Suprofen	<1 mg/mL	52 mg/mL	52 mg/mL
S1713	Piroxicam	<1 mg/mL	66 mg/mL	1 mg/mL
S1328	Etodolac	<1 mg/mL	58 mg/mL	58 mg/mL
S1645	Ketoprofen	<1 mg/mL	51 mg/mL	51 mg/mL
S1903	Diclofenac Sodium	14 mg/mL	64 mg/mL	64 mg/mL
S1518	Ibuprofen Lysine	71 mg/mL	<1 mg/mL	<1 mg/mL
S2047	Lornoxicam	<1 mg/mL	3 mg/mL	<1 mg/mL
S1646	Ketorolac	<1 mg/mL	75 mg/mL	75 mg/mL
S1626	Naproxen Sodium	50 mg/mL	3 mg/mL	<1 mg/mL
S1576	Sulfasalazine (NSC 667219)	<1 mg/mL	80 mg/mL	''<1 mg/mL
S2903	Lumiracoxib	<1 mg/mL	59 mg/mL	'<1 mg/mL
S2531	Asaraldehyde	<1 mg/mL	39 mg/mL	16 mg/mL
S1960	Pranoprofen	<1 mg/mL	51 mg/mL	''6 mg/mL
S2410	Paeoniflorin (NSC 178886)	96 mg/mL	96 mg/mL	'96 mg/mL
S3008	Zaltoprofen	<1 mg/mL	60 mg/mL	31 mg/mL
S2602	Acemetacin	<1 mg/mL	83 mg/mL	58 mg/mL
S1959	Tolfenamic Acid	<1 mg/mL	52 mg/mL	<1 mg/mL
S4049	Valdecoxib	<1 mg/mL	63 mg/mL	18 mg/mL
S2577	Phenacetin	<1 mg/mL	36 mg/mL	36 mg/mL
S2040	Nimesulide	<1 mg/mL	62 mg/mL	<1 mg/mL
S4149	Amfenac Sodium Monohydrate	59 mg/mL	59 mg/mL	4 mg/mL
S4248	Bromfenac Sodium	71 mg/mL	71 mg/mL	'2 mg/mL
S4051	Nabumetone	<1 mg/mL	46 mg/mL	25 mg/mL
S3018	Niflumic acid	<1 mg/mL	56 mg/mL	<1 mg/mL
S3173	Antipyrine	38 mg/mL	38 mg/mL	38 mg/mL
S2121	Licofelone (ML3000)	<1 mg/mL	19 mg/mL	''4 mg/mL
S9190	Oroxin B	-1 mg/mL	100 mg/mL	-1 mg/mL
S3200	Triflusal	<1 mg/mL	50 mg/mL	50 mg/mL
S4011	Ampiroxicam	<1 mg/mL	90 mg/mL	<1 mg/mL
S9208	Ginsenoside Rb3	-1 mg/mL	100 mg/mL	-1 mg/mL
S5177	Naproxen	-1 mg/mL	46 mg/mL	-1 mg/mL
S0931	Jaceosidin	<1 mg/mL	66 mg/mL	'''6 mg/mL
S5418	Parecoxib Sodium	-1 mg/mL	78 mg/mL	'-1 mg/mL
S3969	Veratric acid	-1 mg/mL	36 mg/mL	'-1 mg/mL
S8433	NS-398 (NS398)	<1 mg/mL	62 mg/mL	<1 mg/mL
S0821	Pamicogrel	<1 mg/mL	45 mg/mL	'''<1 mg/mL
S4032	Bismuth Subsalicylate	<1 mg/mL	0.04 mg/mL	<1 mg/mL
S0759	FPL 62064	<1 mg/mL	53 mg/mL	'''20 mg/mL
S5698	Ketorolac tromethamine salt	75 mg/mL	75 mg/mL	8 mg/mL
S0761	Desmethyl Celecoxib	<1 mg/mL	73 mg/mL	'''73 mg/mL
S4628	(+/-)-Sulfinpyrazone	<1 mg/mL	80 mg/mL	'64 mg/mL
S0766	RHC 80267	<1 mg/mL	79 mg/mL	''''79 mg/mL
S4136	Carprofen	<1 mg/mL	55 mg/mL	55 mg/mL
S3063	Diclofenac Diethylamine	<1 mg/mL	74 mg/mL	74 mg/mL
S5640	Ethyl caffeate	-1 mg/mL	41 mg/mL	-1 mg/mL
S3974	(+)-Catechin hydrate	-1 mg/mL	58 mg/mL	-1 mg/mL
S4656	Parecoxib	<1 mg/mL	74 mg/mL	2 mg/mL
S6615	ATB 346	<1 mg/mL	73 mg/mL	<1 mg/mL
S4609	Diflunisal	<1 mg/mL	50 mg/mL	'20 mg/mL
S4176	Trometamol	24 mg/mL	2 mg/mL	<1 mg/mL
S5520	Phenidone	-1 mg/mL	32 mg/mL	-1 mg/mL
S9029	Prim-o-glucosylcimifugin	-1 mg/mL	93 mg/mL	-1 mg/mL
S3931	Ginsenoside Rd	-1 mg/mL	90 mg/mL	-1 mg/mL
S5019	Indobufen	-1 mg/mL	59 mg/mL	-1 mg/mL
S4078	Mefenamic Acid	<1 mg/mL	48 mg/mL	<1 mg/mL
S4651	Etoricoxib	<1 mg/mL	71 mg/mL	'46 mg/mL
S9386	Polygalacic acid	-1 mg/mL	100 mg/mL	-1 mg/mL
S2595	FK-3311	<1 mg/mL	68 mg/mL	8 mg/mL
S6850	NE 52-QQ57	<1 mg/mL	12 mg/mL	'50 mg/mL
S6073	Diclofenac acid	-1 mg/mL	59 mg/mL	-1 mg/mL
S4765	Syringaldehyde	-1 mg/mL	36 mg/mL	-1 mg/mL
S5010	Indometacin Sodium	-1 mg/mL	87 mg/mL	-1 mg/mL
S2995	4-Hydroxyphenylpyruvic acid	<1 mg/mL	36 mg/mL	'''36 mg/mL
S4230	Oxaprozin	<1 mg/mL	59 mg/mL	27 mg/mL
S2349	Rutaecarpine	<1 mg/mL	24 mg/mL	<1 mg/mL
S2272	Indoprofen	<1 mg/mL	52 mg/mL	<1 mg/mL
S4360	Tolmetin Sodium	63 mg/mL	<1 mg/mL	10 mg/mL
S2351	Salicin	24 mg/mL	57 mg/mL	<1 mg/mL
S4526	Fenbufen	<1 mg/mL	50 mg/mL	50 mg/mL
S3899	Hederagenin	-1 mg/mL	94 mg/mL	-1 mg/mL
S9502	Madecassic acid	-1 mg/mL	100 mg/mL	-1 mg/mL
S4539	Salicylic acid	<1 mg/mL	27 mg/mL	27 mg/mL
S9149	Benzoylpaeoniflorin	-1 mg/mL	100 mg/mL	-1 mg/mL
S6685	Mavacoxib	<1 mg/mL	77 mg/mL	77 mg/mL
S4509	4-Aminoantipyrine	40 mg/mL	40 mg/mL	40 mg/mL
S3261	Myrislignan	-1 mg/mL	100 mg/mL	-1 mg/mL
S3872	Guaiacol	-1 mg/mL	24 mg/mL	-1 mg/mL
S5309	Propyphenazone (4-Isopropylantipyrine)	-1 mg/mL	46 mg/mL	-1 mg/mL
S7889	Xanthohumol	<1 mg/mL	70 mg/mL	'70 mg/mL
S3304	Stylopine	-1 mg/mL	2.5 mg/mL	-1 mg/mL
S2108	Flunixin Meglumin	98 mg/mL	98 mg/mL	8 mg/mL
S6780	TFAP	<1 mg/mL	56 mg/mL	56 mg/mL
S3255	Pectolinarigenin	-1 mg/mL	100 mg/mL	-1 mg/mL
S5711	Deracoxib	<1 mg/mL	80 mg/mL	20 mg/mL
S3925	(-)-Epicatechin gallate	-1 mg/mL	88 mg/mL	-1 mg/mL
S3283	Marmesin	-1 mg/mL	100 mg/mL	-1 mg/mL
S4295	Meclofenamate Sodium	63 mg/mL	63 mg/mL	'''63 mg/mL
S6686	SC-560	<1 mg/mL	70 mg/mL	70 mg/mL
S3168	cis-Resveratrol	<1 mg/mL	46 mg/mL	'''46 mg/mL

亜型選択性的な製品

COX製品

All (110) COX阻害剤(109) COX活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1261	Celecoxib (SC 58635) Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.	Cancer Cell, 2021, 39(7):973-988.e9 Clin Cancer Res, 2021, 27(21):5961-5978 J Immunother Cancer, 2021, 9(6)e002305	Reduced hepatic lipid contents and alleviated liver injury in EC-AMPK mice treated with selective COX-2 inhibitors. Wild-type and EC-AMPK mice given a high fat diet were treated with vehicle, celecoxib or nimesulide for a period of 4 weeks. At the end of treatment, parameters including body weight and circulating glucose (A), serum triglyceride and cholesterol levels (B were measured and presented as percentage comparisons against those from vehicle-treated wild-type mice. *P < 0.05 versus wild-type mice treated with vehicle; #P < 0.05 versus EC-AMPK mice treated with vehicle, n = 3-5.
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.	Adv Sci (Weinh), 2021, e2103360 Front Immunol, 2021, 12:685523 Int J Mol Sci, 2021, 22(5)2354	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
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
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
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	Indicated PN and MES spheres were shown expressing GFP under the control of a 7 × TCF/LEF optimal promoter cassette (7 × TOP) and constitutively expressed nuclear mCherry. PN 84 and MES 1123 were treated with Wnt3a (200 ng/ml), indomethacin (Indo; 20 μM), or a control (vehicle). Scale bar, 100 μm. Bar graph, quantification of fluorescent signal of GFP (TOP-GFP) versus mCherry (PGK-H2BmCherry). The percentage of GFP- and mCherry-positive spheres was determined by FACS.
S5786^新	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.
S4435^新	Metamizole sodium hydrate Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties.
S5192^新	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.
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, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58	(d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; P<0.05; *P<0.01.
S3043	Rofecoxib Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM.	Toxicol Appl Pharmacol, 2015, 285(1):51-60
S1734	Meloxicam Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.	PLoS One, 2020, 13;15(3):e0230272 Oncol Lett, 2017, 14(2):2198-2206	Meloxicam (0.25 μg/ml) decreases the migration of CF41.Mg cells. Incubation with 0.25 μg/ml meloxicam for 24 and 48 h inhibited the migration of cells compared with the DMSO‑treated control cells in a wound healing assay. A total of 6 repeats were performed and results are presented as the mean ± standard deviation. Representative images of the wound healing assay and quantification if the results are presented. Scale bar, 90 μm. *P<0.05 vs. the control group.
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.	Cell Rep, 2021, 36(2):109360 Mol Cancer, 2021, 20(1):84 JCI Insight, 2021, 6(19)e147038	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
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	(a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm.
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	TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3).
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.	Dev Cell, 2021, S1534-5807(21)00485-8 Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021 Int Immunopharmacol, 2021, 95:107558
S1761	Suprofen Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
S1713	Piroxicam Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.
S1328	Etodolac Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.
S1645	Ketoprofen Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.	J Nucl Med, 2020, jnumed.120.249367
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.	Arch Toxicol, 2018, 92(6):1953-1967 Cell, 2016, 167(7):1803-1813 Head Neck, 2014, 10.1002/hed.23822
S1518	Ibuprofen Lysine Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
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.
S1646	Ketorolac Ketorolac (Ketorolac tromethamine) 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
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
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 Metab, 2021, S1550-4131(21)00233-3 Sci Adv, 2021, 7(35)eabj0364 Sci Adv, 2021, 7(27)eabh3032
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.	Int J Biol Macromol, 2021, 187:603-613 Cells, 2020, 9(9)E2005 J Am Heart Assoc, 2020, 9(1):e013470	(A) Western blot analysis of MITF expression in MelIM. One representative experiment out of two is shown. (B) Proliferation of MelIM cells under diclofenac or lumiracoxib (0.1 mM) for 3 vs. 30 days. Results are given as percentage of untreated controls.
S2531	Asaraldehyde Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
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
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, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Immunopharmacol Immunotoxicol, 2021, 1-9
S3008	Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
S2602	Acemetacin Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
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
S4049	Valdecoxib Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.	Biochem Bioph Res Co, 2015, 460(2):198-204	(B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot.
S2577	Phenacetin Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties.
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	Nimesulide has no effect on KSHV lytic replication in BCBL-1 cells. The cells induced with TPA for 3 h were treated with the test compounds for 72 h. Then, the effect of nimesulide on cell viability (C) and the number of DNA copies (D) were measured as described in the Methods. CDV (20 µM) is a positive control for inhibiting viral DNA replication. Data were normalized as the fold change compared with the no-TPA induced control. The results are presented as the mean values with standard deviations (n = 3).
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.
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.
S4051	Nabumetone Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
S3018	Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.	Oncol Lett, 2020, 20(4):39
S3173	Antipyrine Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor.
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
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 is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.	J Cancer, 2021, 12(7):2140-2150
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
S4011	Ampiroxicam Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
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).
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
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.
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).
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.
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.
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.
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.	Mol Oncol, 2021, 10.1002/1878-0261.13077 Oxid Med Cell Longev, 2021, 2021:7394344 J Cell Mol Med, 2021, 25(20):9597-9608	(C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.
S0821	Pamicogrel Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties.
S4032	Bismuth Subsalicylate Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
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.
S5698	Ketorolac tromethamine salt Ketorolac 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
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.
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
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).
S4136	Carprofen Carprofen inhibits canine COX2 with IC50 of 30 nM.
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.
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.
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.	J Steroid Biochem Mol Biol, 2021, 211:105906
S4656	Parecoxib Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor.	Theranostics, 2020, 10(8):3366-3381
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.
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.
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.
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.
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.
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
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.
S4078	Mefenamic Acid Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2.	Brain Res, 2020, 20;1740:146846
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
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.
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.
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).
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.	Biosci Biotechnol Biochem, 2020, 18;1-8 Cell Death Dis, 2019, 10(5):358 Dev Cell, 2018, 46(4):441-455.e8
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.
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.
S5010	Indometacin Sodium Indomethacin Sodium (Indometacin 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
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.
S4230	Oxaprozin Oxaprozin 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.
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
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
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.
S4360	Tolmetin Sodium Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids.
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
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
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.
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.
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.
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.
S9149	Benzoylpaeoniflorin Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro.
S6457	Flurbiprofen Axetil Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase.
S6685	Mavacoxib Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID).
S4509	4-Aminoantipyrine 4-Aminoantipyrine(Ampyrone, NSC 60242, Metapirazone, Solnapyrin-A, Solvapyrin-A, Minoazophene, Aminoazophene) 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.
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.
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.
S5309	Propyphenazone (4-Isopropylantipyrine) Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity.
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.	Int J Mol Sci, 2021, 22(22)12134 J-Cancer, 2020, 6;11-14-:4047-4058 Oncol Rep, 2020, 44(4):1365-1374
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.
S2108	Flunixin Meglumin Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.
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.
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).
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).
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
S3283	Marmesin Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity.
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.	Nature, 2019, 573(7775):539-545
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.
S3168^新	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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1261	Celecoxib (SC 58635) Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.	Cancer Cell, 2021, 39(7):973-988.e9 Clin Cancer Res, 2021, 27(21):5961-5978 J Immunother Cancer, 2021, 9(6)e002305	Reduced hepatic lipid contents and alleviated liver injury in EC-AMPK mice treated with selective COX-2 inhibitors. Wild-type and EC-AMPK mice given a high fat diet were treated with vehicle, celecoxib or nimesulide for a period of 4 weeks. At the end of treatment, parameters including body weight and circulating glucose (A), serum triglyceride and cholesterol levels (B were measured and presented as percentage comparisons against those from vehicle-treated wild-type mice. *P < 0.05 versus wild-type mice treated with vehicle; #P < 0.05 versus EC-AMPK mice treated with vehicle, n = 3-5.
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.	Adv Sci (Weinh), 2021, e2103360 Front Immunol, 2021, 12:685523 Int J Mol Sci, 2021, 22(5)2354	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
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
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
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	Indicated PN and MES spheres were shown expressing GFP under the control of a 7 × TCF/LEF optimal promoter cassette (7 × TOP) and constitutively expressed nuclear mCherry. PN 84 and MES 1123 were treated with Wnt3a (200 ng/ml), indomethacin (Indo; 20 μM), or a control (vehicle). Scale bar, 100 μm. Bar graph, quantification of fluorescent signal of GFP (TOP-GFP) versus mCherry (PGK-H2BmCherry). The percentage of GFP- and mCherry-positive spheres was determined by FACS.
S5786^新	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.
S4435^新	Metamizole sodium hydrate Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties.
S5192^新	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.
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, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58	(d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; P<0.05; *P<0.01.
S3043	Rofecoxib Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM.	Toxicol Appl Pharmacol, 2015, 285(1):51-60
S1734	Meloxicam Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.	PLoS One, 2020, 13;15(3):e0230272 Oncol Lett, 2017, 14(2):2198-2206	Meloxicam (0.25 μg/ml) decreases the migration of CF41.Mg cells. Incubation with 0.25 μg/ml meloxicam for 24 and 48 h inhibited the migration of cells compared with the DMSO‑treated control cells in a wound healing assay. A total of 6 repeats were performed and results are presented as the mean ± standard deviation. Representative images of the wound healing assay and quantification if the results are presented. Scale bar, 90 μm. *P<0.05 vs. the control group.
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.	Cell Rep, 2021, 36(2):109360 Mol Cancer, 2021, 20(1):84 JCI Insight, 2021, 6(19)e147038	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
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	(a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm.
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	TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3).
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.	Dev Cell, 2021, S1534-5807(21)00485-8 Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021 Int Immunopharmacol, 2021, 95:107558
S1761	Suprofen Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
S1713	Piroxicam Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.
S1328	Etodolac Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.
S1645	Ketoprofen Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.	J Nucl Med, 2020, jnumed.120.249367
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.	Arch Toxicol, 2018, 92(6):1953-1967 Cell, 2016, 167(7):1803-1813 Head Neck, 2014, 10.1002/hed.23822
S1518	Ibuprofen Lysine Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
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.
S1646	Ketorolac Ketorolac (Ketorolac tromethamine) 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
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
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 Metab, 2021, S1550-4131(21)00233-3 Sci Adv, 2021, 7(35)eabj0364 Sci Adv, 2021, 7(27)eabh3032
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.	Int J Biol Macromol, 2021, 187:603-613 Cells, 2020, 9(9)E2005 J Am Heart Assoc, 2020, 9(1):e013470	(A) Western blot analysis of MITF expression in MelIM. One representative experiment out of two is shown. (B) Proliferation of MelIM cells under diclofenac or lumiracoxib (0.1 mM) for 3 vs. 30 days. Results are given as percentage of untreated controls.
S2531	Asaraldehyde Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
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
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, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Immunopharmacol Immunotoxicol, 2021, 1-9
S3008	Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
S2602	Acemetacin Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
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
S4049	Valdecoxib Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.	Biochem Bioph Res Co, 2015, 460(2):198-204	(B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot.
S2577	Phenacetin Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties.
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	Nimesulide has no effect on KSHV lytic replication in BCBL-1 cells. The cells induced with TPA for 3 h were treated with the test compounds for 72 h. Then, the effect of nimesulide on cell viability (C) and the number of DNA copies (D) were measured as described in the Methods. CDV (20 µM) is a positive control for inhibiting viral DNA replication. Data were normalized as the fold change compared with the no-TPA induced control. The results are presented as the mean values with standard deviations (n = 3).
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.
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.
S4051	Nabumetone Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
S3018	Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.	Oncol Lett, 2020, 20(4):39
S3173	Antipyrine Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor.
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
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 is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.	J Cancer, 2021, 12(7):2140-2150
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
S4011	Ampiroxicam Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
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).
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
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.
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).
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.
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.
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.
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.	Mol Oncol, 2021, 10.1002/1878-0261.13077 Oxid Med Cell Longev, 2021, 2021:7394344 J Cell Mol Med, 2021, 25(20):9597-9608	(C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.
S0821	Pamicogrel Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties.
S4032	Bismuth Subsalicylate Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
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.
S5698	Ketorolac tromethamine salt Ketorolac 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
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.
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
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).
S4136	Carprofen Carprofen inhibits canine COX2 with IC50 of 30 nM.
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.
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.
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.	J Steroid Biochem Mol Biol, 2021, 211:105906
S4656	Parecoxib Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor.	Theranostics, 2020, 10(8):3366-3381
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.
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.
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.
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.
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.
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
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.
S4078	Mefenamic Acid Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2.	Brain Res, 2020, 20;1740:146846
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
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.
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.
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).
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.	Biosci Biotechnol Biochem, 2020, 18;1-8 Cell Death Dis, 2019, 10(5):358 Dev Cell, 2018, 46(4):441-455.e8
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.
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.
S5010	Indometacin Sodium Indomethacin Sodium (Indometacin 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
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.
S4230	Oxaprozin Oxaprozin 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.
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
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
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.
S4360	Tolmetin Sodium Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids.
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
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
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.
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.
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.
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.
S9149	Benzoylpaeoniflorin Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro.
S6457	Flurbiprofen Axetil Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase.
S6685	Mavacoxib Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID).
S4509	4-Aminoantipyrine 4-Aminoantipyrine(Ampyrone, NSC 60242, Metapirazone, Solnapyrin-A, Solvapyrin-A, Minoazophene, Aminoazophene) 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.
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.
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.
S5309	Propyphenazone (4-Isopropylantipyrine) Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity.
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.	Int J Mol Sci, 2021, 22(22)12134 J-Cancer, 2020, 6;11-14-:4047-4058 Oncol Rep, 2020, 44(4):1365-1374
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.
S2108	Flunixin Meglumin Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.
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.
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).
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).
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
S3283	Marmesin Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity.
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.	Nature, 2019, 573(7775):539-545
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.

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S3168^新	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.

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S3168^新

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.

研究分野別

製品類型

COX

シグナル伝達経路

研究分野

阻害剤の選択性比較

亜型選択性的な製品

COX製品