GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.
体外研究
GGTI-2154 inhibits the transfer of geranylgeranyl from [H]GGPP to H-Ras CVLL, with an IC50 of 21 nM.
体内研究
GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice.
GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%.