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编 号:F564985
分子式:C16H22O2
分子量:246.34
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生物活性:
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.

体外研究:
GK563 (0.091 M) inhibits the activity of 100% GVIA iPLA2, 88% GVIA cPLA2 and 25% GV sPLA2.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.GK563 (0-0.1 μM) shows a better inhibitory effect than fluoroketone FKGK18 to GVIA iPLA2 with an IC50 value of 1 nM.GK563 (0-0.1 μM; 16 h) reduces β-cell apoptosis induced by proinflammatory cytokines.
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