|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|
|S5177||Naproxen||-1 mg/mL||46 mg/mL||-1 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|
Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
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.
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.
Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.
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.
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.
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.
(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.
Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2.
Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro.
Parecoxib Sodium is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2).
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.
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).
Phenidone, a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer.
Rofecoxib is a COX-2 inhibitor with IC50 of 18 nM.
Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.
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.
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.
Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.
(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.
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.
Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
Piroxicam is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.
Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.
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.
Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
Lornoxicam is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis.
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.
Naproxen Sodium is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.
Lumiracoxib is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.
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.
Asaraldehyde is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.
Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM.
Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.
(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.
Phenacetin is a non-opioid analgesic without anti-inflammatory properties.
Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.
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).
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.
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.
Nabumetone is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Antipyrine is an analgesic and antipyretic agent; selective COX-3 inhibitor.
Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
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.
Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
Sulfinpyrazone is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.
Carprofen inhibits canine COX2 with IC50 of 30 nM.
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.
Parecoxib is a selective COX2 inhibitor.
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.
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.
Mefenamic Acid is a competitive inhibitor of COX-1 and COX-2.
Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.
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.
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.
Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor.
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.
Fenbufen is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.
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.
Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Phase 1.
Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.
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.