Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid -FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation. FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 uM. It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase -PPMTase) in cell-free systems with a Ki value of 2.6 uM, it is relatively ineffective at inhibiting methylation in whole cells. Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.
產(chǎn)品描述
An inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation; inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 uM