345885

GGTI-2147

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

• Sinonimo/i: GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
• Formula empirica (notazione di Hill): C₂₈H₃₀N₄O₃
• Numero CAS: 191102-87-1
• Peso molecolare: 470.56
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• product name: GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).
• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic)
• Colore: off-white
• Solubilità: DMSO: 200 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable