| Bioactivity | Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx[1][2]. | |||||||||
| Invitro | In RBL 2H3 and bone marrow-derived mast cells (BMMCs), Ca2+ entry is critical for exocytosis. Bromoenol lactone inhibits exocytosis when stimulated using a Ca2+ ionophore A23187, which passively transports Ca2+ down a concentration gradient and also in permeabilised mast cells where Ca2+ entry is no longer relevant. Moreover, Bromoenol lactone has only a minor effect on antigen- or thapsigargin-stimulated Ca2+ signalling, both the release from internal stores and sustained elevation due to Ca2+ influx[1]. | |||||||||
| Name | Bromoenol lactone | |||||||||
| CAS | 88070-98-8 | |||||||||
| Formula | C16H13BrO2 | |||||||||
| Molar Mass | 317.18 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
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| Reference | [1]. Fensome-Green A, et al. Bromoenol lactone, an inhibitor of Group V1A calcium-independent phospholipase A2 inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx. Cell Calcium. 2007 Feb;41(2):145-53. [2]. Takuma T, et al. Role of Ca2+-independent phospholipase A2 in exocytosis of amylase from parotid acinar cells. J Biochem. 1997 Jun;121(6):1018-24. |
Bromoenol lactone
CAS: 88070-98-8 F: C16H13BrO2 W: 317.18
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-indep
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