Chemical Name: (2R,3S,4R)-3-Hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxy-N-acetyl-L-cysteine thioester
Biological ActivityA 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).
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Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells.
Omura et al.
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin.
Fenteany et al.
Inhibition of NF-κB activity induces apoptosis in murine hepatocytes.
Bellas et al.
Citations for Lactacystin
The citations listed below are publications that use Tocris products. Selected citations for Lactacystin include:
6 Citations: Showing 1 - 6
Evaluation of Machine Learning Classifiers to Predict Compound Mechanism of Action When Transferred across Distinct Cell Lines.
Authors: Warchal Et al.
SLAS Discov 2019;24:224
The ubiquitin-proteasome system functionally links neuronal Tomosyn-1 to dendritic morphology.
Authors: Saldate Et al.
J Biol Chem 2018;293:2232
FBG1 Is the Final Arbitrator of A1AT-Z Degradation.
Authors: Wen Et al.
PLoS One 2015;10:e0135591
Glucocorticoid regulates TrkB protein levels via c-Cbl dependent ubiquitination: a decrease in c-Cbl mRNA in the prefrontal cortex of suicide subjects.
Authors: Pandya Et al.
A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory.
Authors: Ren Et al.
CDK5 is essential for soluble amyloid β-induced degradation of GKAP and remodeling of the synaptic actin cytoskeleton.
Authors: Roselli Et al.
PLoS One 2011;6:e23097
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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.