Inhibitor SourceBook™ Second Edition

Lipid Signaling
Cyclooxygenase (COX) Inhibitors, continued
fibrils. Several epidemiological studies have indeed
shown that groups of people taking NSAIDs, for
unrelated conditions, such as rheumatoid arthritis,
have a reduced incidence of Alzheimer's disease. More
recently, coxibs, highly selective COX-2 inhibitors, have
been linked to abnormalities in vascular function and
regulation of hemostatis/thrombosis. This has rekindled
interest in several other COX-2 inhibitors for pain
management.
Cyclooxygenase (COX) Inhibitors
References:
Fries, S., and Grosser, T., 2005. Hematology 445.
Brune, K., and Hinz, B. 2004. Scand. J. Rheumatol. 33, .
Johnson, A.J., et al. 200 . Adv. Enzyme Regul. 41, 22 .
McGeer, P.L., and McGeer, E.G. 200 . Neurobiol. Aging 22, 799.
Schnitzer, T.J. 200 . Am. J. Med. 110 (Suppl ), S46.
Thomas, T., et al. 200 . NeuroReport 12, 3263.
Weggen, S., et al. 200 . Nature 414, 2 2.
Crofford, L.J., et al. 2000. Arthritis Rheum. 43, 4.
Fournier, D.B., et al. 2000. J. Cell Biochem. 77, 97.
Sugaya, K., et al. 2000. Jpn. J. Pharmacol. 82, 85.
Product Cat. No. Comments Size Price
COX- Inhibitor, FR 22047 236005 {4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole,
Hydrochloride; 1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4methylpiperazine,
Hydrochloride; FR 122047}
A potent, cell-permeable and selective inhibitor of COX- (IC 50 = 28 nM; human
recombinant COX- ). Does not significantly inhibit COX-2 (IC 50 = 65 mM; human
recombinant COX-2).
COX-2 Inhibitor I 236011 {LM-1685; Methyl [5-methylsulfonyl-1-(4-chlorobenzyl)-1H-2indolyl]carboxylate}
A potent and selective inhibitor of COX-2 (IC 50 = 650 nM from human
monocytes). Displays only very weak activity against COX- from human
platelets (IC 50 > 0 mM) and in whole blood (IC 50 > 00 mM).
COX-2 Inhibitor II 236012 {4-[(5-Difluoromethyl-3-phenyl)-4-isoxazolyl]benzenesulfonamide; SC-791}
A cell-permeable isoxazolyl-benzenesulfonamide compound that acts as a
potent and highly selective inhibitor of COX-2 both in vitro (IC 50 = 4 nM for
hCOX-2 vs. 4 mM for hCOX- ) and in vivo.
Curcumin, Curcuma longa L. 239802 [1,7-Bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione]
Inhibitor of 5-LOX (IC 50 = 8 mM) and COX (IC 50 = 52 mM). Exhibits antitumor
and anti-inflammatory properties.
Diclofenac, 4'-Hydroxy- 287845 {2-[((2´,6´-Dichloro-4´-hydroxy)phenyl)amino]benzeneacetic Acid; 4´-OHD}
A metabolite of Diclofenac (Cat. No. 287840). Formed through oxidation of
diclofenac by cytochrome P450 2C9. Specifically blocks COX-2 activity (IC 50 =
6.9 nM).
Diclofenac Sodium 287840 {2-[(2,6-Dichlorophenyl)amino]benzeneacetic Acid, Na}
A potent inhibitor of COX- (IC 50 = 76 nM) and COX-2 (IC 50 = 26 nM). Strongly
inhibits insoluble transthyretin (TTR) amyloid fibril formation.
DuP-697 317500 [5-Bromo-2-(4-fluorophenyl)-3-(4-(methylsulfonyl)phenyl)thiophene]
A potent, irreversible, and time-dependent COX-2 inhibitor. Exhibits over 50-fold
greater inhibitory potency against human and murine recombinant COX-2 (IC 50 =
80 nM and 40 nM at 5 and 0 minutes, respectively) than COX- (IC 50 = 9 mM).
Ebselen 324483 [2-Phenyl-1,2-benzisoselenazol-3(2H)-one; PZ51]
A neuroprotective antioxidant that acts as a non-selective inhibitor of the
cyclooxygenases. An excellent scavenger of peroxynitrite, and a glutathione
peroxidase mimetic.
ETYA 434741 (5,8,11,14-Eicosatetraynoic Acid)
Inhibits COX (ID 50 = 8 mM), 5-LOX (ID 50 = 0 mM), 2-LOX
(ID 50 = 300 nM), and 5-LOX (ID 50 = 200 nM) in whole cells.
More online... www.calbiochem.com/inhibitors/cox
Flurbiprofen 344079 {(±)-2-Fluoro-a-methyl[1,1´-biphenyl]-4-acetic Acid; U-27182}
A non-steroidal anti-inflammatory agent that acts as a potent, but non-selective
COX inhibitor (IC 50 = 5 nM for LPS-induced COX in human peripheral blood cells).
Reduces Ab loads and Congo Red staining in APP+PS transgenic mice.
5 mg $ 30
5 mg $ 73
5 mg $ 8
00 mg $35
00 mg $ 03
g $28
5 mg $ 69
5 mg $64
20 mg $203
00 mg $38
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