BEL Haloenol lactone
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BEL is a selective, potent, irreversible, mechanism-based inhibitor of myocardial cytosolic calcium-independent phospholipase A2 (iPLA2) with a Ki value of 180 nM. BEL induces the proteolysis of procaspase-9 and procaspase-3 and increases cleavage of poly (ADP-ribose) polymerase. BEL also inhibits macrophage iPLA2 in a concentration-dependent manner with an IC50 value of 60 nM and is an effective enzyme-activated irreversible inhibitor of chymotrypsin Ki of 636 nM. Long term treatment with BEL increased annexin-V binding to the cell surface and nuclear DNA damage.
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