FTI 276 TFA是一种有效的蛋白法呢基转移酶 (PFT) 抑制剂。FTI 276针对恶性疟原虫和人体的 IC50 值分别为 0.9 nM 和 0.5 nM。

L-778123 hydrochloride 是 FPTase 和 GGPTase-I 的抑制剂，在酶抑制测定中的 IC50 分别为 2 nM 和 98 nM。

Arglabin is a sesquiterpene gamma-lactone is isolated from Artemisia glabella and an anticancer natural compound.

FTI-277 is an inhibitor of farnesyl transferase (FTase) and a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.

ABT-100 is an orally bioavailable farnesyltransferase inhibitor. ABT-100 inhibited proliferation of cells in vitro carrying oncogenic H-Ras (EJ-1 bladder; IC(50) 2.2 nmol/L), Ki-Ras (DLD-1 colon, MDA-MB-231 breast, HCT-116 colon, and MiaPaCa-2 pancreatic; IC(50) range, 3.8-9.2 nmol/L), and wild-type Ras (PC-3 and DU-145; IC(50), 70 and 818 nmol/L, respectively) as well as clonogenic potential. ABT-100 shows 70% to 80% oral bioavailability in mice. ABT-100 regressed EJ-1 tumors (2-12.5 mg/kg/d s.c., every day for 21 days) and showed significant efficacy in DLD-1, LX-1, MiaPaCa-2, or PC-3 tumor-bearing mice (6.25-50 mg/kg/d s.c. once daily or twice daily orally).

Manumycin A is an antibiotic that acts as a potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity. It inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation which requires farnesylation at the C-terminus for membrane attachment.