FKGK 18

FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2beta activity in cytosolic extracts from INS-1 cells overexpressing iPLA2beta (IC50 = ~50 nM) as well as iPLA2gamma activity in mouse heart membrane fractions (IC50s = ~1-3 µM). It inhibits glucose-induced increases in prostaglandin E2 (PGE2, Cay-14010) production and insulin secretion in human pancreatic islets when used at a concentration of 10 µM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2beta in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.Formal Name: 1,1,1-trifluoro-6-(2-naphthalenyl)-2-hexanone. CAS Number: 1071001-09-6. Molecular Formula: C16H15F3O. Formula Weight: 280.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, PBS (pH 7.2): 2 mg/ml. lambdamax: 225, 271 nm. SMILES: O=C(C(F)(F)F)CCCCC1=CC2=CC=CC=C2C=C1. InChi Code: InChI=1S/C16H15F3O/c17-16(18,19)15(20)8-4-1-5-12-9-10-13-6-2-3-7-14(13)11-12/h2-3,6-7,9-11H,1,4-5,8H2. InChi Key: VCWWTQMRNJSJGC-UHFFFAOYSA-N.