Amino Acid Sequence

Z-Leu-Leu-Leu-al

Biochem/physiol Actions

Reversible: yes

Primary Targetproteasome

Product does not compete with ATP.

Target K_i: 4 nM against proteasome

Target IC₅₀: 3 µM against NF-κB activation

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) which initiates apoptosis. Inhibits NF-kB activation (IC₅₀ = 3 µM). Also reported to increases the survival rate of mesenchymal stem cells following their transplantation.

A potent, reversible, and cell-permeable proteasome inhibitor (K_i = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. Inhibits NF-κB activation (IC₅₀ = 3 µM). Also reported to increases the survival rate of mesenchymal stem cells following their transplantation. Prevents β-secretase cleavage. A 10 mM (1 mg/210 µl) solution of MG-132 (Cat. No. 474791) in DMSO is also available. This material is ≥98% pure by HPLC. A material with ≥95% purity by HPLC (Cat. No. 474787) is also available.

Legal Information

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

Other Notes

Li, Z.W. et al. 2011. Sheng Li Xue Bao. 63, 525.Steinhilb, M.L., et al. 2001. J. Biol. Chem.276, 4476.Meriin, A.B., et al. 1998. J. Biol. Chem. 273, 6373.Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.Klafki, H.W., et al. 1996. J. Biol. Chem.271, 2865.Lee, D.H., and Goldberg, A.L., 1996. J. Biol. Chem.271, 27280.Wiertz, E.J., et al. 1996. Cell84, 769.Jensen, T.J., et al. 1995. Cell 83, 129.Read, M.A., et al. 1995. Immunity2, 493.Rock, K.L., et al. 1994. Cell 78, 761.

Packaging

1, 5, 10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Sequence

Z-Leu-Leu-Leu-CHO

Warning

Toxicity: Standard Handling (A)