Merck, 344930-1MG, Furin Inhibitor I

General description
A peptidyl chloromethylketone that binds irreversibly to the catalytic site of furin and blocks its activity. Hence, it can be used as a high specificity cleavage inhibitor of viral glycoproteins and blocker viral replication. Reported to block the shedding of MT5-MMP by furin and prevent the activation of MT5-MMP. Completely inhibits the cleavage of Boc-RVRR-AMC (50 µM) by purified furin or PACE4. Also inhibits the activity of endothelin converting enzyme and reduces the pro-peptide cleavage of BACE (β-site APP-cleaving enzyme).
A peptidyl chloromethylketone that binds to the catalytic site of furin and blocks its activity. Hence, it can be used as a high specificity cleavage inhibitor of viral glycoproteins and blocker of viral replication. Reported to block the shedding of MT5-MMP by furin and prevent the activation of MT5-MMP. Also shown to reduce the pro-peptide cleavage of BACE (β-site APP-cleaving enzyme).
Biochem/physiol Actions
Product does not compete with ATP.
Reversible: no
Cell permeable: yes
Primary Target
viral glycoproteins
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Decanoyl-Arg-Val-Lys-Arg-CMK
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Capell, A., et al. 2000. J. Biol. Chem. 275, 30849.
Denault, J.B., et al. 1995. FEBS Lett. 362, 276.
Denault, J.B., et al. 1995. J. Cardiovasc. Pharmacol.26, S47.
Garten, W., et al. 1994. Biochimie 76, 217.
Hallenberger, S., et al. 1992. Nature 360, 358.
Stieneke-Gröber, A., et al. 1992. EMBO J. 11, 2407.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)