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

L-778,123 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
253863-00-2
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 CTLL-2 cells (IC50 = 0.81 μM).{41264}  

 

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SKU: 22940 - 5 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 CTLL-2 cells (IC50 = 0.81 μM)

Formal name: 4-[[5-[[4-(3-chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]-benzonitrile, monohydrochloride

Synonyms: 

Molecular weight: 442.3

CAS: 253863-00-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity

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