Description
General description
A potent, cell-permeable, and reversible proteasome inhibitor. Inhibits the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex (MPC; Ki = 460 nM). Does not inhibit the peptidyl-glutamyl peptide hydrolyzing activity of MPC even at concentrations of 200 µM. Also blocks the decay of IκB-α and IκB-β proteins in exponentially growing WEHI 231 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MPC
Product does not compete with ATP.
Reversible: yes
Target Ki: 460 nM against the pituitary multicatalytic proteinase complex (MPC)
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months.
Other Notes
Schauer, S.L., et al. 1998. J. Immunol. 160, 4398.
Orlowski, M., et al. 1997. Biochemistry 36, 13946.
Orlowski, M., et al. 1993. Biochemistry 32, 1563.
Z-Leu-Leu-Phe-CHO
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)