Background:

LB42708 is a selective inhibitor of farnesyltransferase (FTase) with IC50 value of 0.8nM [1].

LB42708 is a nonpeptide pyrrole-based FTase inhibitor with high potency and selectivity. It inhibits the farnesylation of H-ras, N-ras and K-ras4B in vitro with IC50 values of 0.8nM, 1.2nM and 2nM, respectively. To the related enzyme geranylgeranyltransferase I, LB42708 shows no significant inhibition with IC50 value of 100μM. In cultured RAW264.7 cell line, LB42708 potently reduces the farnesylated p21ras stimulated by LPS and IFN-γ with IC50 value of