L-778123

L-778123 is a small molecule dual inhibitor of farnesyl transferase (FTase) and geranylgeranyl transferase type I (GGTase I), enzymes involved in the post-translational prenylation of proteins such as Ras family GTPases. By inhibiting both FTase and GGTase I with high potency (IC50 values of 2 nM for FTase and 98 nM for GGTase I), it blocks the prenylation—and thus activation—of key signaling proteins implicated in cancer cell proliferation. It was developed by Merck Research Laboratories as an antineoplastic agent and has been evaluated primarily in phase I clinical trials for recurrent or refractory solid tumors and lymphomas. Despite its ability to inhibit protein prenylation in preclinical models and human samples, clinical development did not progress beyond early-phase studies due to dose-limiting toxicities[1][3][4][7][8].

Other names

4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile4-[(5-{[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl}-1H-imidazol-1-yl)methyl]benzonitrileL778123L-778123L 778123L778,123