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BEL is a selective, potent, irreversible, mechanism-based inhibitor of myocardial cytosolic calcium-independent phospholipase A2 (iPLA2) with a Ki value of 180 nM.1 BEL also inhibits macrophage iPLA2 in a concentration-dependent manner with an IC50 value of 60 nM and is an effective enzyme-activated irreversible inhibitor of chymotrypsin (Ki = 636 nM).2,3
2
Ackermann, E.J., Conde-Frieboes, K., and Dennis, E.A. Inhibition of macrophage Ca2+-independent phospholipase A2 by bromoenol lactone and trifluoromethyl ketones. J Biol Chem270445-450(1995).
3
Daniels, S.B., Cooney, E., Sofia, M.J., et al. Haloenol lactones. Potent enzyme-activated irreversible inhibitors for α-chymotrypsin. J Biol Chem25815046-15053(1983).
Room temperature
in continental US; may vary elsewhere
SMILES
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Br/C=C1\CCC(C(=O)O\1)c1cccc2ccccc12
Background Reading
Ackermann, E.J., Conde-Frieboes, K., and Dennis, E.A. Inhibition of macrophage Ca2+-independent phospholipase A2 by bromoenol lactone and trifluoromethyl ketones. J Biol Chem270445-450(1995).
Daniels, S.B., Cooney, E., Sofia, M.J., et al. Haloenol lactones. Potent enzyme-activated irreversible inhibitors for α-chymotrypsin. J Biol Chem25815046-15053(1983).
Hazen, S.L., Zupan, L.A., Weiss, R.H., et al. Suicide inhibition of canine myocardial cytosolic calcium-independent phospholipase A2. J Biol Chem2667227-7232(1991).
Bromoenol lactone is available in the following screening
library: