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Biological Activity for Lactacystin
Lactacystin 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).
Technical Data for Lactacystin
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Lactacystin
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Lactacystin
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for Lactacystin
References are publications that support the biological activity of the product.
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
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Keywords: Lactacystin, Lactacystin supplier, Cell-permeable, potent, selective, proteasome, inhibitors, inhibits, Proteasome, Proteinases, Proteases, 2267, Tocris Bioscience
6 Citations for Lactacystin
Citations are publications that use Tocris products. Selected citations for Lactacystin include:
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
Saldate et al (2018) The ubiquitin-proteasome system functionally links neuronal Tomosyn-1 to dendritic morphology. J Biol Chem 293 2232 PMID: 29269412
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
Wen et al (2015) FBG1 Is the Final Arbitrator of A1AT-Z Degradation. PLoS One 10 e0135591 PMID: 26295339
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
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Reviews for Lactacystin
Average Rating: 4 (Based on 1 Review.)
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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.
Literature in this Area
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Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Custom Degrader Services
- Ubiquitin-Proteasome System Proteins and Assays
- Assays for Protein Degradation
Targeted Protein Degradation Poster
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