FKGK18

FKGK18 is a selective group VIA calcium-independent phospholipase A 2 (GVIA iPLA 2 ) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC 50 s of 50 nM and 3 μM for iPLA 2 β and iPLA 2 γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes In Vitro FKGK18 (1 nM; 1 h) inhibits glucose-stimulated insulin secretion (GSIS) and prostaglandin E2 (PGE2) generation. FKGK18 (0.1-10 nM; 24 h) inhibits beta-cell apoptosis. FKGK18 (0.1-10 μM; 24 h) affects immune cells function and influences B-cell survival. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human pancreatic islets Concentration: 1 nM Incubation Time: 1 h Result: Inhibited GSIS from pancreatic islets, AA hydrolysis from beta-cells membranes and PGE2 generation. Penetrated islets and the beta-cells from islets. Apoptosis AnalysisCell Line: INS-1 OE cells Concentration: 0.1-10 nM Incubation Time: 24 h Result: Inhibited beta-cells apoptosis induced by ER-stress. Cell Viability AssayCell Line: CD4 + T-cell and B-cell from 8–12-week-old NOD female mice Concentration: 0.1-10 μM/L Incubation Time: 24 h Result: Decreased TNF-α generation, reduced viability of B cell and antibody production. In Vivo FKGK18 (20 mg/kg; i.p. three times per week from 10 days until euthanasia) reduces diabetes incidence. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 10-day-old female NOD miceDosage: 20 mg/kg Administration: Intraperitoneal injection; 20 mg/kg three times per week; from 10 days until euthanasia Result: Reduced diabetes incidence and maintained better glucose homeostasis. Form:Solid IC50& Target:IC50: 50 nM (iPLA2β), 3 μM (iPLA2γ)

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