Farnesylation involves the utilization of farnesyl pyrophosphate (FPP), an intermediate in the mevalonate pathway, by farnesyltransferase (FTase) to add a lipid, farnesyl, to certain proteins. This post-translational modification is crucial in allowing target proteins, including Ras, to associate with, and function at, membranes. FTase Inhibitor II is a cell-permeable analog of FPP that potently inhibits FTase (IC = 50-75 nM), preventing farnesylation of Ras. It does not inhibit geranylgeranyl transferase at similar concentrations (IC > 100 µM). FTase Inhibitor II displays no toxicity to untransformed cells but blocks Ras-mediated transformation of NIH 3T3 cells.
FTase Inhibitor II is a farnesyltransferase inhibitor, with IC50 values of 150 nM and 1500 nM against FTase and GGTase I, respectively. FTase Inhibitor II is not farnesylated by FTase, thus avoiding metabolic inactivation.
分子式
C15H21N3O4S2
分子量
371.47
CAS号
156707-43-6
中文名称
N-[4-[[(2R)-2-氨基-3-巯基-1-氧代丙基]氨基]苯甲酰基]-L-蛋氨酸
运输条件
Room temperature in continental US; may vary elsewhere.