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Submit ReviewLactacystin is a cell-permeable, potent and selective proteasome inhibitor. A Streptomyces metabolite that is thought to bind irreversibly to the active site N-terminal threonine residue of the catalytic β-subunit of the 20S proteasome, thereby inhibiting its chymotrypsin and trypsin-like activities. Induces neurite outgrowth in Neuro 2a neuroblastoma cells and has been reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 μM).
分子量 | 376.42 |
公式 | C15H24N2O7S |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 133343-34-7 |
PubChem ID | 6610292 |
InChI Key | DAQAKHDKYAWHCG-RWTHQLGUSA-N |
Smiles | O=C1N[C@]([C@@](SC[C@H](NC(C)=O)[C@](O)=O)=O)([C@H](C(C)C)O)[C@@H](O)[C@H]1C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 3.76 | 10 |
以下数据基于产品分子量 376.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 26.57 mL | 132.83 mL | 265.66 mL |
0.5 mM | 5.31 mL | 26.57 mL | 53.13 mL |
1 mM | 2.66 mL | 13.28 mL | 26.57 mL |
5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
参考文献是支持产品生物活性的出版物。
Omura et al (1991) Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells. J.Antibiot. 44 113 PMID: 1848215
Fenteany et al (1995) Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin. Science 268 726 PMID: 7732382
Bellas et al (1997) Inhibition of NF-κB activity induces apoptosis in murine hepatocytes. Am.J.Pathol. 151 891 PMID: 9327720
If you know of a relevant reference for Lactacystin, please let us know.
关键词: Lactacystin, Lactacystin supplier, Cell-permeable, potent, selective, proteasome, inhibitors, inhibits, Proteasome, Proteinases, Proteases, 2267, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Lactacystin 的部分引用包括:
Saldate et al (2018) The ubiquitin-proteasome system functionally links neuronal Tomosyn-1 to dendritic morphology. J Biol Chem 293 2232 PMID: 29269412
Pandya et al (2014) Glucocorticoid regulates TrkB protein levels via c-Cbl dependent ubiquitination: a decrease in c-Cbl mRNA in the prefrontal cortex of suicide subjects. Psychoneuroendocrinology 45 108 PMID: 24845182
Wen et al (2015) FBG1 Is the Final Arbitrator of A1AT-Z Degradation. PLoS One 10 e0135591 PMID: 26295339
Warchal et al (2019) Evaluation of Machine Learning Classifiers to Predict Compound Mechanism of Action When Transferred across Distinct Cell Lines. SLAS Discov 24 224 PMID: 30694704
Ren et al (2013) A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory. Neuropsychopharmacology 38 778 PMID: 23303053
Roselli et al (2011) CDK5 is essential for soluble amyloid β-induced degradation of GKAP and remodeling of the synaptic actin cytoskeleton. PLoS One 6 e23097 PMID: 21829588
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To tested the effects of inhibiting the proteolytic activity of the 26S proteasome complex via bath application of MG132 (50 M, 4 h) or lactacystin (10 M, 4 h) versus DMSO vehicle control.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia