GGTI - 2133, >= 98%( HPLC ), solide

Non disponible en dehors du Royaume-Uni et de l'Irlande

Application

GGTI-2133 has been usedTo understand the role of geranylgeranyl transferase in the regulation of CXC chemokine production and neutrophil recruitment in the lung.To study the importance of geranylgeranylation in cell adhesion.To measure ligand-induced ADP-ribosylation factor 6 (Arf6) activation in breast cancer cells.

Biochem/physiol Actions

GGTI-2133 is a cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I; IC50 = 38 nM) with a 140-fold selectivity over farnesyltransferase (FTase; IC₅₀ = 5.4 µM).

GGTase I mediates prenylation to induce the oncogenic functions of the Ras and Rho proteins. Thus, GGTase I inhibitors can be utilized as effective anticancer drugs. They are also useful in treating inflammation, atherosclerosis, multiple sclerosis and other diseases.

Packaging

1, 5 mg in glass bottle