乳胞素

乳胞素用途

Lactacystin 是一种抗生素,链霉菌属的代谢物,是一种有效的选择性蛋白酶体 (proteasome) 抑制剂,对 20S 蛋白酶体的 IC50 为 4.8 μM。Lactacystin 还抑制溶酶体酶组织蛋白酶 A。Lactacystin 抑制细胞生长并诱导神经突增生。

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乳胞素名称

[ CAS 号 ]:
133343-34-7

[ 中文名 ]:
乳胞素

[ 英文名 ]:
Lactacystin

[英文别名 ]:

(+)-Lactacystin
MFCD01076525
LACTACYSTIN

乳胞素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 4.8 μM (proteasome)[1]

[体内研究]

在年轻和成年小鼠注射后5-7天,乳酸半胱氨酸(微注射; 2μg)诱导帕金森病样运动表型[2]。动物模型：8-9周(年轻)和12-14个月(成年)大的雄性C57Bl/6RccHsd小鼠[2]剂量：2μg给药：微注射结果：在年轻和成年小鼠注射后5-7天诱导帕金森病样运动表型。

[参考文献]

[1]. Csizmadia V, et al. Effect of proteasome inhibitors with different chemical structures on the ubiquitin-proteasomesystem in vitro. Vet Pathol. 2010 Mar;47(2):358-67.

[2]. Savolainen MH, et al. Nigral injection of a proteasomal inhibitor, lactacystin, induces widespread glial cell activationand shows various phenotypes of Parkinson's disease in young and adult mouse. Exp Brain Res. 2017 Jul;235(7):2189-2202.

乳胞素物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
714.9±60.0 °C at 760 mmHg

[ 熔点 ]:
233-235ºC dec.

[ 分子式 ]:
C₁₅H₂₄N₂O₇S

[ 分子量 ]:
376.425

[ 闪点 ]:
386.1±32.9 °C

[ 精确质量 ]:
376.130432

[ PSA ]:
178.33000

[ LogP ]:
-1.10

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±5.2 mmHg at 25°C

[ 折射率 ]:
1.560

[ 储存条件 ]:
−20°C

乳胞素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

乳胞素文献

Neuroprotective effect of modified Chungsimyeolda-tang, a traditional Korean herbal formula, via autophagy induction in models of Parkinson's disease.

J. Ethnopharmacol. 159 , 93-101, (2014)

Previous studies in our laboratory revealed the neuroprotective effect of modified Yeoldahanso-tang (MYH) in models of Parkinson׳s disease (PD). In this study, we investigated another traditional Kore...

Septins arrange F-actin-containing fibers on the Chlamydia trachomatis inclusion and are required for normal release of the inclusion by extrusion.

MBio 5(5) , e01802-14, (2014)

Chlamydia trachomatis is an obligate intracellular human pathogen that grows inside a membranous, cytosolic vacuole termed an inclusion. Septins are a group of 13 GTP-binding proteins that assemble in...

Development of two novel high-throughput assays to quantify ubiquitylated proteins in cell lysates: application to screening of new anti-malarials.

Malaria Journal 14 , 200, (2015)

The ubiquitin proteasome system (UPS) is one of the main proteolytical pathways in eukaryotic cells and plays an essential role in key cellular processes such as cell cycle, stress response, signal tr...

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乳胞素