345885

GGTI-2147

≥95% (HPLC), solid, GGTase I inhibitor, Calbiochem^®

• Synonyme(s) : GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
• Formule empirique (notation de Hill): C₂₈H₃₀N₄O₃
• Numéro CAS: 191102-87-1
• Poids moléculaire : 470.56
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• product name: GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).
• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic)
• Couleur: off-white
• Solubilité: DMSO: 200 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I). Blocks the geranyl-geranylation of Rap1A with an IC₅₀ value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC₅₀ = 500 nM for Rap1A versus IC₅₀ >30 µM for H-Ras).

Methyl ester derivative of GGTI-2133 (Cat. No. 345884). A potent and selective non-thiol inhibitor of geranylgeranyltransferase I (GGTase I) over farnesyltransferase (FTase) in whole cells. Blocks the geranylgeranylation of Rap1A with an IC₅₀ value greater than 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC₅₀ = 500 nM for Rap1A versus IC₅₀<30 µM for H-Ras).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
GGTase-I

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 500 nM in blocking the geranyl-geranylation of Rap1A

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol.41, 316.
Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.

Informations légales

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

Informations sur la sécurité

• 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