弗林蛋白酶抑制剂 I-Calbiochem

C₃₄H₆₆ClN₁₁O₅

744.41

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).

Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Primary Target
viral glycoproteins

Toxicity: Standard Handling (A)

Decanoyl-Arg-Val-Lys-Arg-CMK

Supplied as a trifluoroacetate salt.

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

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.

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

100

≥90% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated

off-white

methanol: 1 mg/mL
DMSO: soluble

ambient

−20℃

1 mg in Plastic ampoule

11 - Combustible Solids

WGK 1