L-778,123

L-778,123 is a dual inhibitor of farnesyl transferase (FTase, IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I, IC50 = 98 nM). It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 µM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 µM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 µM).Formal Name: 4-[[5-[[4-(3-chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]-benzonitrile. CAS Number: 183499-57-2. Molecular Formula: C22H20ClN5O. Formula Weight: 405.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml, Ethanol: 10 mg/ml. SMILES: ClC1=CC(N2C(CN(CC3=CN=CN3CC4=CC=C(C#N)C=C4)CC2)=O)=CC=C1. InChi Code: InChI=1S/C22H20ClN5O/c23-19-2-1-3-20(10-19)28-9-8-26(15-22(28)29)14-21-12-25-16-27(21)13-18-6-4-17(11-24)5-7-18/h1-7,10,12,16H,8-9,13-15H2. InChi Key: JNUGFGAVPBYSHF-UHFFFAOYSA-N.