Lactacystin

Biological Activity

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

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.

Background References

1. Heparan Sulfate Proteoglycans Promote Telomerase Internalization and MHC Class II Presentation on Dendritic Cells
   
   J Immunol, 2016;197(5):1597-608.
2. Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells.
   Omura et al.
   J.Antibiot., 1991;44:113
3. Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin.
   Fenteany et al.
   Science, 1995;268:726
4. Inhibition of NF-κB activity induces apoptosis in murine hepatocytes.
   Bellas et al.
   Am.J.Pathol., 1997;151:891

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