Merck, 539160-5MG, Proteasome Inhibitor I

General description
A cell-permeable, reversible inhibitor of the chymotrypsin-like activity of the multicatalytic proteinase complex (MCP; 20S proteasome) in HT4 cells. Causes the accumulation of ubiquitinated proteins in neuronal cells. Prevents the activation of NF-κB in response to TNF-α and Okadaic Acid (Cat. No. 495604) through inhibition of IκB-α degradation. A 50 mM (5 mg/162 µl) solution of Proteasome Inhibitor I (Cat. No. 539161) in DMSO is also available.
Cell-permeable inhibitor of the chymotrypsin-like activity of the multicatalytic proteinase complex (MCP; 20S proteasome) in HT4 cells. Causes the accumulation of ubiquitinylated proteins in neuronal cells. Prevents NF-κB activation in response to TNFα and okadaic acid through inhibition of IκB-α degradation, thereby interfering with induction of iNOS in macrophages.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Chymotrypsin-like activity of the multicatalytic proteinase complex (MCP; 20S proteasome) in HT4 cells
Product does not compete with ATP.
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 months at -20°C.
Other Notes
Griscavage, J.M., et al. 1996. Proc. Natl. Acad. Sci. USA93, 3308.
Mori, S., et al. 1995. J. Biol. Chem.270, 29447.
Figueiredo-Pereira, M.E., et al. 1994. J. Neurochem. 63, 1578.
Traenckner, E.B., et al. 1994. EMBO J. 13, 5433.
Z-Ile-Glu(OtBu)-Ala-Leu-CHO
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)