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 iPLA2B activity in cytosolic extracts from INS-1 cells overexpressing iPLA2B (IC50 ~50 nM) as well as iPLA2Y activity in mouse heart membrane fractions (IC50 ~1-3 M) inhibits glucose-induced increases in PGE2 production and insulin secretion in human pancreatic islets at 10 M inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2B 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