COX

inhibitors of COX-1 and COX-2

A selective inhibitor of COX-2

CAY10452 (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities.

TFAP is a selective cyclooxygenase-1 (COX-1) inhibitor, with an IC50 of 0.8 uM.

NB-598 is a potent, orally active, and competitive inhibitor of squalene epoxidase (SE).

S-(+)-Marmesin ((+)-Marmesin) is a natural coumarin, exhibiting COX-2/5-LOX dual inhibitory activity.

LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.

A polyphenol with diverse biological activities

Adelmidrol exerts important anti-inflammatory effects that are partly dependent on PPARγ.

A ginsenoside with diverse biological activities

Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis.

Metamizole sodium hydrate is a potent analgesic drug that has been demonstrated to inhibit cyclooxygenase (COX).

A diterpenoid furanolactone with diverse biological activities

RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.

Flosulide (ZK 38997) is a potent and selective COX-2 inhibitor, used for the treatment for inflammatory diseases.

Thioflosulide (L-745337) (L-745337) is a selective cyclooxygenase-2 (COX2) inhibitor, with an IC50 of 2.3 nM, and shows anti-inflammatory activity.

S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.

Methyl Salicylate (Wintergreen oil) (Wintergreen oil) is a topical analgesic and anti-inflammatory agent.

Tilmacoxib (JTE522) (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.

SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM.

COX-2-IN-1 is potent and slective COX-2 inhibitor with an IC50 of 3.9 μM.

Timegadine (SR1368), a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.

COX/5-LO-IN-1 (Atreleuton analog) is an inhibitor of cylooxygenase and 5-lipoxygenase (5-LO), used for the research of inflammatory and allergic disease states.