CAY10502

Phospholipase A₂ (PLA₂) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA₂ (cPLA₂α) 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 PLA₂α (cPLA₂α) with an IC₅₀ 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 IC₅₀ values of 570 and 0.9 nM, respectively.²

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).