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

FKGK 18 – 25 mg

Brand:
Cayman
CAS:
1071001-09-6
Storage:
-20
UN-No:
Non-Hazardous - /

FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2).{21518} 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 iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM).{42790} It inhibits glucose-induced increases in prostaglandin E2 (PGE2; Item No. 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 iPLA2β 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.{42791}  

 

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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

Formal name: 1,1,1-trifluoro-6-(2-naphthalenyl)-2-hexanone

Synonyms: 

Molecular weight: 280.3

CAS: 1071001-09-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Lipid Biochemistry|Glycerophospholipids|Phospholipases

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