L-778,123 (hydrochloride)

L-778,123 (hydrochloride)

CAT N°: 22940
Price:

From 146.00 124.10

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 ?M) 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 ?M, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 ?M).{41264}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-[[5-[[4-(3-chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]-benzonitrile, monohydrochloride
  • Correlated keywords
    • 183499-57-2 FPTase GGPTase-I farnesyl L778 778123 L-778123 CD 71 28 CTLL2 IL2 interleukin HDJ-2 RAP-1A
  • Product Overview:
    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 ?M) 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 ?M, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 ?M).{41264}

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