Description
trans-(±)-GK563 is a potent β-lactone inhibitor of group VIA (GVIA) calcium-independent phospholipase A
2 (GVIA iPLA
2; IC
50 = 1 nM).
1 It is selective for GVIA iPLA
2 over GVIA cPLA
2 (IC
50 = 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).
