344930

Furin Inhibitor I

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

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

Properties

• product name: Furin Inhibitor I, Furin Inhibitor I, is a peptidyl chloromethylketone that binds to the catalytic site of furin and blocks its activity.
• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable