Description
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 (iPLA
2) are a PLA
2 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 (iPLA
2γ). Unlike (S)-
BEL, (R)-
BEL does not inhibit iPLA
2β except at high doses of 20-
30 μM.
2 (R)-
BEL inhibits human recombinant iPLA
2γ with an IC
50 of approximately 0.6 μM.
Uses
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM[1][2].
References
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 iPLA2γ, as the mediator of arginine vasopressin-induced arachidonic acid release in A-10 smooth muscle cells J. Biol. Chem. 277(36),32807-32814(2002).
