| CAS NO: | 88070-98-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 317.2 |
| Cas No. | 88070-98-8 |
| Formula | C16H13BrO2 |
| Solubility | ≤2mg/ml in ethanol;25mg/ml in DMSO;50mg/ml in dimethyl formamide |
| Chemical Name | 6E-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one |
| Canonical SMILES | Br/C=C1\CCC(C(=O)O\1)c1cccc2ccccc12 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Bromoenol lactone is a potent and irreversible inhibitor of myocardial cytosolic calcium-independent phospholipase A2 (iPLA2) [1].
The iPLA2 has been involved in stimulus-induced arachidonic acid release and lysophospholipid generation. The catalytic action of iPLA2 is responsible for phospholipid remodeling as a housekeeping function. Arachidonic acid and lysophospholipid generated by iPLA2 act as a signaling molecule in cellular functions, including eicosanoid production, glucose-induced insulin secretion, Fas-induced apoptosis, cellular proliferation, membrane traffic in fusion, contribution to myocardial ischemia, and others [2].
BEL promoted apoptosis in a variety of cell lines, including U937, THP-1, and MonoMac (human phagocyte), RAW264.7 (murine macrophage), Jurkat (human T lymphocyte), and GH3 (human pituitary). Long term treatment with BEL (up to 24 h) increased annexin-V binding to the cell surface and nuclear DNA damage. BEL induced the proteolysis of procaspase-9 and procaspase-3 and increased cleavage of poly (ADP-ribose) polymerase [1]. BEL inhibited cellular phosphatidic acid phosphohydrolase (PAP) activity in intact P388D1 macrophages with an IC50 of ～8 μM. BEL blocked triacylglycerol biosynthesis in P388D1 cells by decreasing diacylglycerol availability [3].
References:
[1] Fuentes L, Pérez R, Nieto M L, et al. Bromoenol lactone promotes cell death by a mechanism involving phosphatidate phosphohydrolase-1 rather than calcium-independent phospholipase A2[J]. Journal of Biological Chemistry, 2003, 278(45): 44683-44690.
[2] Akiba S, Sato T. Cellular function of calcium-independent phospholipase A2[J]. Biological and Pharmaceutical Bulletin, 2004, 27(8): 1174-1178.
[3] Balsinde J, Dennis E A. Bromoenol lactone inhibits magnesium-dependent phosphatidate phosphohydrolase and blocks triacylglycerol biosynthesis in mouse P388D1 macrophages[J]. Journal of Biological Chemistry, 1996, 271(50): 31937-31941.
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