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Principaux documents

344510

Sigma-Aldrich

FTase Inhibitor I

The FTase Inhibitor I controls the biological activity of FTase. This small molecule/inhibitor is primarily used for Cancer applications.

Synonyme(s) :

FTase Inhibitor I, N-[2(S)-[2(R)-Amino-3-mercaptopropylamino]-3-methylbutyl]-Phe-Met-OH, B581

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About This Item

Formule empirique (notation de Hill):
C22H38N4O3S2
Poids moléculaire :
470.69
Code UNSPSC :
12352200

Niveau de qualité

100

Pureté

≥90% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated (hygroscopic)

Couleur

white

Solubilité

water: 1 mg/mL
DMSO: 5 mg/mL

Conditions d'expédition

ambient

Température de stockage

−20°C

Description générale

A potent, cell-permeable inhibitor of farnesyltransferase (FTase) that is about 37-fold more active against FTase (IC50 = 21 nM in vitro) than against geranylgeranyltransferase (GGTase; IC50 = 790 nM). Very resistant to proteolysis.
A potent, cell-permeable, selective, peptidomimetic inhibitor of farnesyltransferase (FTase) that is approximately 37-fold more active against FTase (IC50 = 21 nM in vitro) than against geranylgeranyltransferase (GGTase; IC50 = 790 nM). Very resistant to proteolysis.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
FTase
Product does not compete with ATP.
Reversible: no
Target IC50: 21 nM against FTase in vitro

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Yamaguchi, M., et al. 2004. Stroke35, 1750.
Cox, A.D., et al. 1994. J. Biol. Chem.269, 19203.
Garcia, A.M., et al. 1993. J. Biol. Chem. 268, 18415.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Carmen M Deveau et al.
Biochemical pharmacology, 183, 114349-114349 (2020-11-28)
Serotonin neurotransmission is largely governed by the regulation of the serotonin transporter (SERT). SERT is modulated in part by cholesterol, but the role of cholesterol and lipid signaling intermediates in regulating SERT are unknown. Serotonergic neurons were treated with statins
Yusuke Marikawa et al.
Molecular human reproduction, 27(4) (2021-03-08)
Early embryos are vulnerable to environmental insults, such as medications taken by the mother. Due to increasing prevalence of hypercholesterolemia, more women of childbearing potential are taking cholesterol-lowering medications called statins. Previously, we showed that inhibition of the mevalonate pathway

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