I-102

Material Data Sheet

clasto-Lactacystin beta Lactone

Price: $1,200.00
Catalog #: I-102

clasto-Lactacystin beta Lactone

Price: 
$1,200
Quantity: 
1 mg
Data Sheet: 
application/pdf icon102_blactone.pdf
Structure: 
Purity: 
95% by HPLC. Structure confirmed by <sup>1</sup>H-NMR.
Solubility: 
Soluble up to 20 mg/ml and stable in DMSO, MeCN. Subject to hydrolysis in aqueous buffers. Pellet dry compound by centrifugation prior to DMSO addition. Store at -20°C. Avoid multiple freeze/thaw cycles.
Activity: 
kobs / [I] = 20,000 M-1 s-1 vs. 20S:PA28 complex. Inhibits ubiquitin proteasome pathway in cell culture (IC50=1 μM).
Potent, highly specific, irreversible and cell-permeable inhibitor that covalently modifies the catalytic β subunits of the proteasome. The β-lactone intermediate is generated from the aqueous hydrolysis of lactacystin, and is the active inhibitory species that reacts with the proteasome.

Literature

References: 

Dick R.L., et al. (1996) J. Biol. Chem. 271:7273-7276
Dick R.L., et al. (1997) J. Biol. Chem. 272:182-188
Craiu A., et al. (1997) J. Biol. Chem. 272:13437-13445
Fenteany G. and Schreiber S.L. (1998) J. Biol. Chem. 273:8545-8548
Fenteany G et al. (1995) Science. 268:726-731
Masse C.E., et al. (2000) Eur. J. Org. Chem. 714:2513-2528