(R)-BEL

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components.¹ The calcium-independent phospholipases (iPLA₂) are a PLA₂ subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA₂γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA₂β except at high doses of 20-30 μM.² (R)-BEL inhibits human recombinant iPLA₂γ with an IC₅₀ of approximately 0.6 μM.

1. Balsinde, J., Balboa, M.A., Insel, P.A., et al. Regulation and inhibition of phospholipase A₂ Annu. Rev. Pharmacol. Toxicol. 39,175-189(1999).
2. Jenkins, C.M., Han, X., Mancuso, D.J., et al. Identification of calcium-independent phospholipase A₂ (iPLA₂)β, and not iPLA_2γ, as the mediator of arginine vasopressin-induced arachidonic acid release in A-10 smooth muscle cells J. Biol. Chem. 277(36),32807-32814(2002).