Methyl ganoderate A, an inhibitor of Farnesyl protein transferase (FPT) with an IC50 of 38 µM, exhibits potential anticancer effects. Additionally, it inhibits fatty acid amide hydrolase (FAAH), further underscoring its therapeutic potential.
FTase-IN-1 (compound 17a) is a highly effective inhibitor of fanesyl transferase (FTase), exhibiting a remarkable IC50 value of 0.35 μM. This compound demonstrates significant cytotoxicity potential and exhibits powerful antitumor activity [1].
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyltransferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyltransferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).