GGTI 2418 is an inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 9.5 nM).1 It is selective for GGTase I over farnysltransferase (FTase; IC50 = 53,000 nM). GGTI 2418 (100 mg/kg) reduces tumor growth in an MDA-MB-231 breast cancer mouse xenograft model.
1.Kazi, A., Carie, A., Blaskovich, M.A., et al.Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: Implications for breast cancer therapyMol. Cell Biol.29(8)2254-2263(2009)