溴烯醇内酯

溴烯醇内酯用途

Bromoenol lactone ((6E)-Bromoenol lactone) 是一种不可逆的选择性的和有效的钙依赖性磷脂酶 A2 (iPLA2β) 抑制剂,其 IC50 值约为 7 μM,可抑制抗原刺激的肥大细胞胞吐作用,而不会阻止 Ca2+ 的大量涌入。

溴烯醇内酯名称

[ CAS 号 ]:
88070-98-8

[ 中文名 ]:
溴烯醇内酯

[ 英文名 ]:
HELSS

[英文别名 ]:

Haloenol lactone suicide substrate
MFCD00270871
bromoenol lactone
6-Btnpo
L66J B- FT6VOYTJ CU1E
HELSS
BEL
BTNP

溴烯醇内酯生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 其他

[ 靶点 ]

PLA2:7 μM (IC50)

[体外研究]

在RBL 2H3和骨髓来源的肥大细胞(BMMC)中,Ca2+进入对胞吐作用至关重要。当使用Ca2+离子载体A23187刺激时,溴代醇内酯抑制胞吐作用,Ca2+离子载体A23187被动地将Ca2+转运至浓度梯度,并且还在Ca2+进入不再相关的透化肥大细胞中。此外,溴代醇内酯对抗原或毒胡萝卜素刺激的Ca2+信号传导仅有轻微影响,包括内部储存的释放和由于Ca2+流入引起的持续升高[1]。

[参考文献]

[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.

溴烯醇内酯物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
467.0±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₆H₁₃BrO₂

[ 分子量 ]:
317.177

[ 闪点 ]:
236.2±28.7 °C

[ 精确质量 ]:
316.009888

[ PSA ]:
26.30000

[ LogP ]:
4.36

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.716

[ 储存条件 ]:
-20°C

溴烯醇内酯MSDS

详细MSDS(安全技术说明书)

溴烯醇内酯安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

溴烯醇内酯文献

Persistent Nociception Triggered by Nerve Growth Factor (NGF) Is Mediated by TRPV1 and Oxidative Mechanisms.

J. Neurosci. 35 , 8593-603, (2015)

Nerve growth factor (NGF) is elevated in certain chronic pain conditions and is a sufficient stimulus to cause lasting pain in humans, but the actual mechanisms underlying the persistent effects of NG...

Bromoenol Lactone Attenuates Nicotine-Induced Breast Cancer Cell Proliferation and Migration.

PLoS ONE 10 , e0143277, (2015)

Calcium independent group VIA phospholipase A2 (iPLA2β) and Matrix Metalloproteinase-9 (MMP-9) are upregulated in many disease states; their involvement with cancer cell migration has been a recent su...

Cytosolic phospholipase A2 plays a crucial role in ROS/NO signaling during microglial activation through the lipoxygenase pathway.

J. Neuroinflammation 12 , 199, (2015)

Oxidative stress and inflammation are important factors contributing to the pathophysiology of numerous neurological disorders, including Alzheimer's disease, Parkinson's disease, acute stroke, and in...

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