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Merck

344930

Furin Inhibitor I

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

Synonyme(s) :

Furin Inhibitor I, Decanoyl-RVKR-CMK

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A propos de cet article

Formule empirique (notation de Hill) :
C34H66ClN11O5
Poids moléculaire :
744.41
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥90% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated
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Nom du produit

Furin Inhibitor I, Furin Inhibitor I, is a peptidyl chloromethylketone that binds to the catalytic site of furin and blocks its activity.

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

Quality Level

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

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
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

Disclaimer

Toxicity: Standard Handling (A)

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Consulter la Bibliothèque de documents

Zhujun Ao et al.
iScience, 25(8), 104759-104759 (2022-07-21)
The Delta variant had spread globally in 2021 and caused more serious disease than the original virus and Omicron variant. In this study, we investigated several virological features of Delta spike protein (SPDelta), including protein maturation, its impact on viral
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Nature communications, 13(1), 3482-3482 (2022-06-18)
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Journal of lipid research, 62, 100003-100003 (2021-01-12)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates cholesterol metabolism by inducing the degradation of hepatic low density lipoprotein receptors (LDLRs). Plasma PCSK9 has 2 main molecular forms: a 62 kDa mature form (PCSK9_62) and a 55 kDa, furin-cleaved form (PCSK9_55).
Montalbano Mauro et al.
International journal of molecular sciences, 24(13) (2023-07-14)
Glypican-3 (GPC-3) is a heparin sulfate proteoglycan located extracellularly and anchored to the cell membrane of transformed hepatocytes. GPC-3 is not expressed in normal or cirrhotic liver tissue but is overexpressed in hepatocellular carcinoma (HCC). Because of this, GPC-3 is
Xiaoyang Yu et al.
Antiviral research, 211, 105552-105552 (2023-02-04)
HBV cccDNA is the persistent form of viral genome, which exists in host cell nucleus as an episomal minichromosome decorated with histone and non-histone proteins. cccDNA is the authentic viral transcription template and resistant to current antivirals. Growing evidence shows

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