Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Target K_i: 460 nM against the pituitary multicatalytic proteinase complex (MPC)

Primary TargetMPC

Cell permeable: yes

General description

A potent, cell-permeable, and reversible proteasome inhibitor. Inhibits the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex (MPC; K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

1, 5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months.

Sequence

Z-Leu-Leu-Phe-CHO

Warning

Toxicity: Standard Handling (A)