Lactacystin (Synthetic)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Lactacystin是一种特异性的和不可逆的蛋白酶体抑制剂，其IC50值为4.8 μM[1]。
Lactacystin结合到20S蛋白酶体的催化亚基，抑制蛋白酶体的所有三个肽酶活性：胰凝乳蛋白酶样、胰蛋白酶样和caspase样活性。利用此特性，Lactacystin用于研究蛋白酶体的作用。在Neuro-2a细胞中，给予Lactacystin诱导神经突生长以及引起短暂性cAMP水平升高和细胞的双极形态。在MG-63人骨肉瘤细胞中，Lactacystin也可以抑制细胞周期进程。此外，据报道，Lactacystin有效治疗神经胶质瘤细胞。在大鼠C6神经胶质瘤细胞中，Lactacystin显著抑制细胞生长，其IC50值约为10 μM。在神经胶质瘤异种移植小鼠模型中，给予1~5 μg/20 g剂量的Lactacystin可以减少肿瘤体积[2，3]。
参考文献：
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.
- 1. Xiaozhou Li, Ye Yang, et al. "Chitosan hydrogel loaded with recombinant protein containing epitope C from HSP90 of Candida albicans induces protective immune responses against systemic candidiasis." Int J Biol Macromol. 2021 Mar 15;173:327-340. PMID:33482211
- 2. Yunkai Yang, Xiaohan Guo, et al. "Generated SecPen_NY-ESO-1_ubiquitin-pulsed dendritic cell cancer vaccine elicits stronger and specific T cell immune responses." Acta Pharmaceutica Sinica B Available online 25 August 2020.
- 3. Mukhopadhyay U, Chanda S, et al. "Bi-phasic regulation of RNA interference during Rotavirus infection by modulation of Argonaute2." Cell Microbiol. 2019 Aug 19:e13101. PMID:31424151
- 4. 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
| Storage | Store at -20°C |
| M.Wt | 376.42 |
| Cas No. | 133343-34-7 |
| Formula | C15H24N2O7S |
| Solubility | Soluble in H2O |
| Chemical Name | 2-acetamido-3-[3-hydroxy-2-(1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1C(C(NC1=O)(C(C(C)C)O)C(=O)SCC(C(=O)O)NC(=O)C)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。 |
| 细胞实验 [1]: | |
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细胞系 |
C6细胞 |
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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。 |
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反应条件 |
2.5、5或10 μM |
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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]: | |
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动物模型 |
携带神经胶质瘤的裸鼠 |
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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 |
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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。 |
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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。 |
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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. |
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化学结构
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