货号 | 10010501-5mg |
描述 | 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.1 FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 µM.2 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 µM, it is relatively ineffective at inhibiting methylation in whole cells.3 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.4 |
别名 | FTS;Salirasib; |
供应商 | Cayman |
应用文献 | |
1.Haklai, R.,Weisz, M.G.,Elad, G., et al. Dislodgment and accelerated degradation of ras. Biochemistry 37, 1306-1314 (1998). 2.Marciano, D.,Ben-Baruch, G.,Marom, M., et al. Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth. Journal of Medicinal Chemistry 38, 1267-1272 (1995). 3.Marom, M.,Haklai, R.,Ben-Baruch, G., et al. Selective inhibition of ras-dependent cell growth by farnesylthiosalicylic acid. The Journal of Biological Chemisty 270(38), 22263-22270 (1995). 4.George, J.,Afek, A.,Keren, P., et al. Functional inhibition of ras by S-trans, trans-farnesyl thiosalicylic acid attenuates atherosclerosis in apolipoprotein E knockout mice. Circulation 105, 2416-2422 (2002). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥96% |
计算分子量 | 358.5 |
分子式 | C22H30O2S |
CAS号 | 162520-00-5 |
稳定性 | ≥ 2 years |
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