(±)-trans-GK563

GK563 is a selective Ca2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

IC50: 1 nM (GVIA iPLA2), 22 μM (GVIA cPLA2)[1]

GK563 (0.091 M) inhibits the activity of 100% GVIA iPLA2, 88% GVIA cPLA2 and 25% GV sPLA2[1]. GK563 (0-0.1 μM) inhibits GVIA iPLA2 with a XI(50) value of 0.0000021 and inhibits GVIA cPLA2 with an IC50 value of 22 μM[1]. GK563 (0-0.1 μM) shows a better inhibitory effect than fluoroketone FKGK18 to GVIA iPLA2 with an IC50 value of 1 nM[1]. GK563 (0-0.1 μM; 16 h) reduces β-cell apoptosis induced by proinflammatory cytokines[1]. Apoptosis Analysis[1] Cell Line: β-cell line Concentration: 0.1-10 μM Incubation Time: 16 h Result: Promoted a slight but modest rise in cell death when worked alone, but produced a concentration-dependent inhibition of β-cell apoptosis by the co-treatment of cells with cytokines.