FKGK 18

An inhibitor of GVIA iPLA2; inhibits GVIA iPLA2 by 99.9% at 0.091 mol fraction in a mixed micelle activity assay; is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively; inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50 = ~1-3 µM); inhibits glucose-induced increases in PGE2 production and insulin secretion in human pancreatic islets at 10 µM; inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner; reduces blood glucose levels in an intraperitoneal glucose tolerance test and incidence of diabetes and increases serum insulin levels in NOD mice at 20 mg/kg, 3 times per week