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 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. Biochem Biophys Acta17611246-1259(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 Chem492611-2620(2006).
Schaloske, R.H., and Dennis, E.A. The phospholipase A2 superfamily and its group numbering system. Biochem Biophys Acta17611246-1259(2006).
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 Chem492611-2620(2006).
CAY10502 is available in the following screening
library: