FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.

Tipifarnib (IND 58359; R115777) is a potent and specific farnesyltransferase inhibitor with an IC50 of 0.6 nM.

FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM for FT-1 and GGT-1, respectively.

FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.

Ftase inhibitor III is an anion-dependent Farnesyltransferase inhibitor from a phenotypic screen.

Zaragozic acid B, a fungal metabolite, is a potent inhibitor of both farnesyl-protein transferase (FPTase) and squalene synthases. Zaragozic acid B is a potential anticancer drug.

Zaragozic acid E, a fungal metabolite, is a potent inhibitor of squalence synthetase with IC50s of 2.3-28 nM.