A dual inhibitor of FTase and GGTase I (IC50s = 2 and 98 nM

L-778,123 – 50 mg

Brand:
Cayman
CAS:
183499-57-2
Storage:
-20
UN-No:
Non-Hazardous - /

L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} 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).{41264}  

 

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SKU: 32504 - 50 mg Category:

Description

A dual inhibitor of FTase and GGTase I (IC50s = 2 and 98 nM, respectively); inhibits prenylation of FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively); inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner; reduces HDJ2 and Rap1a prenylation ex vivo in dog PBMCs when administered at a dose of 35-50 mg/kg per day; has no effect on Ki-Ras prenylation in patient-derived PBMCs; inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively); 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

Synonyms: 

Molecular weight: 405.9

CAS: 183499-57-2

Purity: ≥95%

Formulation: A crystalline solid

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