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Sigma-Aldrich

Furin Inhibitor I

≥90% (HPLC), solid, furin inhibitor, Calbiochem®

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Synonym(s):
Furin Inhibitor I, Decanoyl-RVKR-CMK
Empirical Formula (Hill Notation):
C34H66ClN11O5
Molecular Weight:
744.41
UNSPSC Code:
12352200
NACRES:
NA.28

Quality Level

Assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated

color

off-white

solubility

methanol: 1 mg/mL
DMSO: soluble

shipped in

ambient

storage temp.

−20°C

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

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

Warning

Toxicity: Standard Handling (A)

Sequence

Decanoyl-Arg-Val-Lys-Arg-CMK

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.

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.

Legal Information

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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