bromoenol lactone

Bromoenol lactone ((6E)-Bromoenol lactone) is a selective calcium-dependent phospholipase A2 (iPLA2β) and serine protease inhibitor that attenuates nicotine-induced breast cancer cell proliferation and migration, inhibits voltage-gated Ca2+ and transient receptor potential classical channels, and inhibits carrageenan-induced prostaglandin production and hyperalgesia in rat hind paws.

(R)-Bromoenol lactone is an irreversible, chiral and mechanism-based iPLA2γ inhibitor, with an IC50 of approximately 0.6 µM against human recombinant iPLA2γ.

(S)-Bromoenol lactone is a chiral, mechanism-based irreversible inhibitor targeting calcium-independent phospholipase A2(iPLA2). Compared with its enantiomer (R)-BEL, (S)-Bromoenol lactone has higher selectivity for iPLA2γ(Group VIB), and it is often used in combination with (R)-BEL to distinguish the functions of different subtypes of iPLA2 in arachidonic acid release and cell signal transduction.