| Description | Bromoenol lactone is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β; IC50: ~7 μM). It inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx. |
| In vitro | Bromoenol lactone inhibits exocytosis when stimulated using a Ca2+ ionophore A23187, which passively transports Ca2+ down a concentration gradient and also in permeabilized mast cells where Ca2+ entry is no longer relevant. In RBL 2H3 and bone marrow-derived mast cells (BMMCs), Ca2+ entry is critical for exocytosis. Moreover, Bromoenol lactone has only a minor effect on antigen- or thapsigargin-stimulated Ca2+ signaling, both the release from internal stores and sustained elevation due to Ca2+ influx [1]. |
| Target activity | PLA2:7 μM |
| Synonyms | (6E)-Bromoenol lactone |
| molecular weight | 317.18 |
| Molecular formula | C16H13BrO2 |
| CAS | 88070-98-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 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. |