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Lactacystin (Synthetic)

现货
Catalog No.
A2583
蛋白酶体抑制剂
组合的产品项目
规格价格库存 数量
100ug
¥ 720.00
Ship with 10-15 days
500ug
¥ 3,040.00
Ship with 10-15 days
1mg
¥ 5,320.00
Ship with 10-15 days

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Background

Lactacystin is a specific and an irreversible inhibitor of proteasome with IC50 value of 4.8 μM [1].

Lactacystin binds to the catalytic subunits of the 20 S proteasome and inhibits all the three peptidase activities of the proteasome, chymotrypsin-like, trypsin-like and caspase-like. With this feature, lactacystin is used to study the role of the proteasome. In Neuro-2a cells, lactacystin treatment resulted in the induction of neurite outgrowth. It caused a transient increase in cAMP levels and the bipolar morphology of the cells. Lactacystin also inhibited cell cycle progression in MG-63 human osteosarcoma cells. Moreover, lactacystin was reported to have therapeutic effects on glioma cells. In rat C6 glioma cells, lactacystin significantly inhibited cell growth with IC50 value of about 10 μM. Besides that, in a mouse gliomaxenograft model, administration of lactacystin resulted in tumor size reduction at a dose of 1-5 μg / 20 g body weight [2, 3].

References:
1. Csizmadia V, Csizmadia E, Silverman L, et al. Effect of proteasome inhibitors with different chemical structures on the ubiquitin–proteasome system in vitro. Veterinary Pathology Online, 2010, 47(2): 358-367.
2. Fenteany G, Schreiber S L. Lactacystin, proteasome function, and cell fate. Journal of Biological Chemistry, 1998, 273(15): 8545-8548.
3. Wang H, Zhang S, Zhong J, et al. The proteasome inhibitor lactacystin exerts its therapeutic effects on glioma via apoptosis: An in vitro and in vivo study. Journal of International Medical Research, 2013, 41(1): 72-81.

文献引用

1. Zheng Y, Liu Q, t al. "Zika virus elicits inflammation to evade antiviral response by cleaving cGAS via NS1-caspase-1 axis." EMBO J. 2018 Jul 31. pii: e99347. PMID:30065070

Chemical Properties

StorageStore at -20°C
M.Wt376.42
Cas No.133343-34-7
FormulaC15H24N2O7S
SolubilitySoluble in H2O
Chemical Name2-acetamido-3-[3-hydroxy-2-(1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid
SDFDownload SDF
Canonical SMILESCC1C(C(NC1=O)(C(C(C)C)O)C(=O)SCC(C(=O)O)NC(=O)C)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

试验操作

细胞实验 [1]:

细胞系

C6细胞

制备方法

在无菌水中的溶解度为10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

2.5、5或10 μM

实验结果

与对照组相比,Lactacystin于3个指定剂量下显著抑制C6细胞增殖。此外,与对照组相比,Lactacystin在上述浓度下也能显著增加凋亡细胞数量和降低线粒体膜电位。

动物实验 [1]:

动物模型

携带神经胶质瘤的裸鼠

给药剂量

每20 g体重给予1.0 μg或5.0 μg;腹腔注射;每天1次,持续7天

实验结果

在携带神经胶质瘤的裸鼠中,Lactacystin显著抑制肿瘤生长。然而,在第17天,所有实验组的肿瘤体积恢复到基线水平。于终止Lactacystin治疗后的第9天,肿瘤染色结果显示,Lactacystin显著增加Bax与Bcl-2的mRNA和蛋白质水平的比值。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Wang H, Zhang S, Zhong J, et al. The proteasome inhibitor lactacystin exerts its therapeutic effects on glioma via apoptosis: An in vitro and in vivo study. Journal of International Medical Research, 2013, 41(1): 72-81.

质量控制

质量控制和MSDS

批次:

化学结构

Lactacystin (Synthetic)

相关生物数据

Lactacystin (Synthetic)