Drug intelligence / Profile preview

lactacystin

Development stage
Preclinical
Lead developer
Kitasato Institute
Modality
Small Molecules
Administration
Laboratory Use (experimental), Not Approved For Clinical Human Administration
01

Overview

**Lactacystin** is a naturally occurring metabolic product of *Streptomyces* species, first identified in 1991. It is a cell-permeable, potent, and irreversible **proteasome inhibitor** with high selectivity for the 20S proteasome. Lactacystin acts by covalently binding to the N-terminal threonine residue of β-subunits of the proteasome, thereby inhibiting its chymotrypsin-like, trypsin-like, and caspase-like peptidase activities. Its active transformation product, clasto-lactacystin β-lactone (also known as omuralide), mediates this covalent modification. Lactacystin is extensively used as a biochemical research tool for studies on proteasome function, protein degradation, and cell cycle regulation. It is not approved for therapeutic use in humans. There is interest in its potential as an anticancer agent and as a model for neurodegenerative disease research[1][3][4][7][9][10].

Other names
133343-34-7CHEBI:52722N-acetyl-S-({(2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxopyrrolidin-2-yl}carbonyl)-L-cysteine(2R)-2-acetamido-3-[(2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid
02

Targets

PSMB1 (26S Proteasome (β1-Subunit))PSMB7 (Proteasome subunit beta type-7)PSMB5 (Proteasome subunit beta Type-5)

Beyond the preview

Go deeper on lactacystin.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on lactacystin.

Gosset Free

Get started with Gosset.

Enter your corporate email.

Work email preferred.

Book a call