Merck, 474791-1MG, MG-132

General description
Potent, reversible, and cell-permeable proteasome inhibitor (Ki = 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).
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: 3 µM in inhibiting NF-κB activation
Target Ki: 4 nM as proteasome inhibitor
Packaging
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)