(±)-trans-GK563 Chemical Properties

Boiling point:

364.2±11.0 °C(Predicted)

Density 

1.010±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Chloroform: slightly soluble; DMSO: slightly soluble; Methanol: slightly soluble

(±)-trans-GK563 Usage And Synthesis

Description

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).