Description
Phospholipase A
2 (PLA
2) catalyzes the hydrolysis of phospholipids at the
sn-
2 position leading to the production of lysophospholipids and free fatty acids. Calcium-
dependent cytosolic PLA
2 (cPLA
2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway.
1 CAY10502 is a potent inhibitor of calcium-
dependent cytosolic PLA
2α (cPLA
2α) with an IC
50 value of 4.3 nM for the purified enzyme from human platelets.
2 It inhibits arachidonic acid mobilization from A23187-
stimulated or TPA-
stimulated human platelets with IC
50 values of 570 and 0.9 nM, respectively.
2
References
1. Schaloske, R.H., and Dennis, E.A.
The phospholipase A2 superfamily and its group numbering system Biochim. Biophys. Acta 1761,1246-1259(2006).
2. Ludwig, J., Bovens, S., Brauch, C., et al.
Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2α J. Med. Chem. 49,2611-2620(2006).