(±)-trans-GK563

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.

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].

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).