Biological Activity
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
| M. Wt | 376.42 |
| Formula | C15H24N2O7S |
| Storage | Desiccate at -20°C |
| 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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 3.76 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 376.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.66 mL | 13.28 mL | 26.57 mL |
| 5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Lactacystin, supplier, Cell-permeable, potent, selective, proteasome, inhibitors, inhibits, Proteasome, Proteinases, Proteases, Proteasome, Proteasome, Tocris Bioscience
