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trans-(±)-GK563 is a potent β-lactone inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (GVIA iPLA2; IC50 = 1 nM).1 It is selective for GVIA iPLA2 over GVIA cPLA2 (IC50 = 22 μM). trans-(±)-GK563 (1 and 10 μM) inhibits apoptosis induced by IL-1β and IFN-γ in INS-1 β-cells. | [References]
1. Dedaki, C., Kokotou, M.G., Mouchlis, V.D., et al. β-Lactones: A novel class of Ca2+-independent phospholipase A2 (group VIA iPLA2) inhibitors with the ability to inhibit β-cell apoptosis J. Med. Chem. 62(6),2916-2927(2019). |
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