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Description: Cell-permeable, potent and selective proteasome inhibitor
Chemical Name: (2R,3S,4R)-3-Hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxy-N-acetyl-L-cysteine thioester
Purity: ≥95% (HPLC)
Citations (6)
Reviews (1)
Literature (2)

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

M. Wt 376.42
Formula C15H24N2O7S
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 133343-34-7
PubChem ID 6610292
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

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
water 3.76 10

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Lactacystin

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for Lactacystin, please let us know.

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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:

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

Do you know of a great paper that uses Lactacystin from Tocris? Please let us know.

Reviews for Lactacystin

Average Rating: 4 (Based on 1 Review.)

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lactacystin (10 M, 4 h).
By Anonymous on 12/23/2019
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: rat hippocampal neuronal

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.

PMID: 29269412
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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Targeted Protein Degradation Research Product Guide

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
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Targeted Protein Degradation Poster

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