Amino Acid Sequence

Z-Leu-Leu-Leu-al

Biochem/physiol Actions

Target IC₅₀: 3 µM in inhibiting NF-κB activation

Reversible: yes

Product does not compete with ATP.

Target K_i: 4 nM as proteasome inhibitor

Cell permeable: yes

General description

Potent, reversible, and cell-permeable proteasome inhibitor (K_i = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable stains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1) and inhibits NF-κB activation (IC₅₀ = 3 µM).

Legal Information

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

Other Notes

Meriin, A.B., et al. 1998. J. Biol. Chem.273, 6373.Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.Lee, D.H., and Goldberg, A.L. 1996. J. Biol. Chem.271, 27280.Wiertz, E.J.H.J., et al. 1996. Cell84, 769.Read, M.A., et al. 1995. Immunity2, 493.Rock, K.L., et al. 1994. Cell78, 761.

Packaging

1, 5 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (1 mg/210 µl) or (5mg/1050 µl) solution of MG-132 (Cat. No. 474790) in DMSO.

Warning

Toxicity: Irritant (B)