Biochem/physiol Actions
Reversible: no
Primary Targetviral glycoproteins
Product does not compete with ATP.
Cell permeable: yes
General description
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).
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).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Sugrue, R.J., et al. 2001. J. Gen. Virol.82, 1375.Wang, X., and Pei, D. 2001. J. Biol. Chem.276, 35953.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.
Packaging
1 mg in Plastic ampoule
Physical form
Supplied as a trifluoroacetate salt.
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Sequence
Decanoyl-Arg-Val-Lys-Arg-CMK
Warning
Toxicity: Standard Handling (A)
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