COX

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1261	Celecoxib	<1 mg/mL	76 mg/mL	33 mg/mL
S1255	Nepafenac	<1 mg/mL	50 mg/mL	<1 mg/mL
S1638	Ibuprofen	<1 mg/mL	41 mg/mL	41 mg/mL
S1723	Indomethacin	<1 mg/mL	72 mg/mL	24 mg/mL
S2007	Sulindac	<1 mg/mL	71 mg/mL	9 mg/mL
S5418	Parecoxib Sodium	-1 mg/mL	78 mg/mL	-1 mg/mL
S5010	Indometacin Sodium	-1 mg/mL	87 mg/mL	-1 mg/mL
S5711	Deracoxib	<1 mg/mL	80 mg/mL	20 mg/mL
S5520	Phenidone	-1 mg/mL	32 mg/mL	-1 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
S3017	Aspirin	<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
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
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
S4011	Ampiroxicam	<1 mg/mL	90 mg/mL	<1 mg/mL
S8433	NS-398 (NS398)	<1 mg/mL	62 mg/mL	<1 mg/mL
S4032	Bismuth Subsalicylate	<1 mg/mL	0.04 mg/mL	<1 mg/mL
S4628	(+/-)-Sulfinpyrazone	<1 mg/mL	80 mg/mL	64 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
S4656	Parecoxib	<1 mg/mL	74 mg/mL	2 mg/mL
S4609	Diflunisal	<1 mg/mL	50 mg/mL	20 mg/mL
S4176	Trometamol	24 mg/mL	2 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
S4230	Oxaprozin	<1 mg/mL	59 mg/mL	27 mg/mL
S2349	Rutaecarpine	<1 mg/mL	24 mg/mL	<1 mg/mL
S2351	Salicin	24 mg/mL	57 mg/mL	<1 mg/mL
S4526	Fenbufen	<1 mg/mL	50 mg/mL	50 mg/mL
S4539	Salicylic acid	<1 mg/mL	27 mg/mL	27 mg/mL
S7889	Xanthohumol	<1 mg/mL	70 mg/mL	70 mg/mL
S2108	Flunixin Meglumin	98 mg/mL	98 mg/mL	8 mg/mL
S4295	Meclofenamate Sodium	63 mg/mL	63 mg/mL	63 mg/mL

Isoform-specific Inhibitors

COX Inhibitors (57)
New COX Products

Catalog No.	Information	Product Use Citations	Product Validations
S1261	Celecoxib Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.	Sci Transl Med, 2018, 10(433) Blood, 2011, 118(22):5891-900 Br J Pharmacol, 2014, 171(2):498-508	Tumors were resected from mice 10 days after orthotopic inoculation of 4T1-Luc2 cells, and hydrogels loaded with the following payloads were evaluated: anti–PD-1, anti-CTLA-4, IL-15sa, lenalidomide, celecoxib, STING-RR, or R848. Mice that did not receive a hydrogel were examined as a negative control. (A) IVIS imaging of 4T1-Luc2 cells is shown for all groups described and illustrates tumor burden.
S1255	Nepafenac Nepafenac 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.
S1638	Ibuprofen Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.
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.	Nat Commun, 2016, 7:12885 Theranostics, 2017, 7(5):1389-1406	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.
S2007	Sulindac Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.	Oncogene, 2017, 36(6):787-796 Oncogene, 2016, 10.1038/onc.2016.247	(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.
S5418^New	Parecoxib Sodium Parecoxib Sodium is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2).
S5010^New	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.
S5711^New	Deracoxib Deracoxib 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).
S5520^New	Phenidone Phenidone, a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer.
S3043	Rofecoxib Rofecoxib 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.	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 is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.		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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 Oncotarget, 2016, 7(37):59388-59401	(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.
S3017	Aspirin Aspirin 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.	Toxicol Appl Pharmacol, 2015, 285(1):51-60
S1761	Suprofen Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
S1713	Piroxicam Piroxicam 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 is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.
S1903	Diclofenac Sodium Diclofenac Sodium 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.	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 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.
S1626	Naproxen Sodium Naproxen Sodium is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.
S2903	Lumiracoxib Lumiracoxib is a novel, selective COX-2 inhibitor with K_i of 0.06 μM. It also inhibits COX1 with K_i of 3 μM.	Biochem Pharmacol, 2017, 135:139-150 Xenobiotica, 2016, 10.1080/00498254.2016.1206239	Blood concentration-time profiles for lumiracoxib following single oral administration at 10 mg/kg to (a) Hu-FRGTM mice (n = 3) and (b) to Mu-FRGTM mice (n = 3). Symbols represent concentration-time profiles from individual animals.
S2531	Asaraldehyde Asaraldehyde is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
S1960	Pranoprofen Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
S3008	Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
S2602	Acemetacin Acemetacin 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.
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 is a non-opioid analgesic without anti-inflammatory properties.
S2040	Nimesulide Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.	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 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 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.
S3173	Antipyrine Antipyrine is an analgesic and antipyretic agent; selective COX-3 inhibitor.
S4011	Ampiroxicam Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
S8433	NS-398 (NS398) NS-398 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.		(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.
S4032	Bismuth Subsalicylate Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
S4628	(+/-)-Sulfinpyrazone Sulfinpyrazone is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.
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.
S4656	Parecoxib Parecoxib is a selective COX2 inhibitor.
S4609	Diflunisal Diflunisal 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.
S4078	Mefenamic Acid Mefenamic Acid is a competitive inhibitor of COX-1 and COX-2.
S4651	Etoricoxib Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.
S4686	Vitamin E Vitamin E 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.
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.
S2349	Rutaecarpine Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor.
S2351	Salicin Salicin 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.
S4526	Fenbufen Fenbufen is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.
S4539	Salicylic acid Salicylic acid is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
S7889	Xanthohumol Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Phase 1.
S2108	Flunixin Meglumin Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic 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.

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COX

Signaling Pathway Map

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Isoform-specific Inhibitors