clasto-Lactacystin beta-lactone CAS: 155975-72-7
MF: C10H15NO4
MW: 213.23
A 20S proteasome and cathepsin A inhibitor.

clasto-Lactacystin β-lactone (CAS 155975-72-7)

clasto-Lactacystin β-lactone | CAS 155975-72-7 is rated 5.0 out of 5 by 1.
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Synonym: Omuralide; clasto-Lactacystin |A-lactone; Clasto-lactacystin(Omuralide)
Application: A 20S proteasome and cathepsin A inhibitor
CAS Number: 155975-72-7
Purity: >95%
Molecular Weight: 213.23
Molecular Formula: C10H15NO4
* Refer to Certificate of Analysis for lot specific data (including water content).
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clasto-Lactacystin β-lactone, a synthetic derivative of lactahydrin, is a cell permeable, irreversible and specific inhibitor of the 20S proteasome involved in the ubiquitin-proteasome degradation pathway. Kinetic studies indicate that clasto-Lactacystin β-lactone interacts with the proteasome at its catalytic site threonines, which opens the β-lactone ring and allows the proteasome's catalytic hydroxyl group to become acylated. clasto-Lactacystin β-lactone has been reported to rapidly enter cells in mammalian cell culture media and to additionally inactivate the proteasome in Jurkat cells in a dose-dependent manner. In addition, clasto-Lactacystin β-lactone is reported to inhibit cathepsin A, lead to adipogenesis and induce neurite growth in rat PC12 cells.


References

1. Fenteany, G., et al. 1995. Science. 268: 726-731. PMID: 7732382
2. Dick, L.R., et al. 1997. J. Biol. Chem. 272: 182-188. PMID: 8995245
3. Obin, M., et al. 1999. J. Biol. Chem. 274: 11789-11795. PMID: 10206996
4. Kisselev, A.F., et al. 2001. Chem. Biol. 8: 739-758. PMID: 11514224

Usage :
Soluble in DMSO. DMSO stock solutions can be diluted using a pH 7 buffer, however do not use after one day due to gradual hydrolysis in aqueous media. Store at -20C for up to two years, and protect from light.
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), and acetonitrile.
Storage :
Store at -20° C
Melting Point :
161.31° C (Predicted)
Boiling Point :
440.82° C at 760 mmHg
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.52 (Predicted)
IC50 :
Oryctolagus cuniculus: IC50 = 57 nM; Ubiquitin proteasome pathway: IC50 = 1 µM; HEK293: IC50 = 1.6 µM (human); RPMI-8226: IC50 = 3.3 µM (human)
pK Values :
pKa: 13.33 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
PubChem CID :
9794358
MDL Number :
MFCD01076526
SMILES :

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Certificate of Analysis

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clasto-Lactacystin beta-lactone  Product Citations

See how others have used clasto-Lactacystin beta-lactone. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 28261569  Rucks, EA. et al. 2017. Frontiers in cellular and infection microbiology. 7: 40.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Felsenberg J; et al Felsenberg J; et al. (PubMed ID: 25063852) determined that clasto-Lactacystin β-lactone, a proteasome inhibitor, blocks the activity of the proteasome in honeybee brains and enhances the long term memory retention in olfactory conditioning. -SCBT Publication Review
Date published: 2015-02-05
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