Cysmethynil
货号：
14745-5mg 基本售价：
910.0 元 规格：
5 mg
产品信息
概述| 货号 | 14745-5mg |
| 描述 | Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. Cysmethynil is an indole-based, time-dependent inhibitor of Icmt (IC50=<200 nM).1 It acts as a competitive inhibitor with respect to the isoprenylated cysteine substrate and a noncompetitive inhibitor with respect to S-adenosylmethionine (Ki = 0.14 µM for the final complex).2 It does not inhibit other enzymes in the prenylation pathway (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 µM, or related methyltransferases.1 Treatment of cancer cells results in a dose-dependent decrease in Ras carboxylmethylation, mislocalization of Ras, and impaired signaling through Ras pathways.1 Treatment of PC3 prostate cancer cells with 25 µM cysmethynil resulted in decreased mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death.3 |
| 别名 | Icmt Inhibitor; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Winter-Vann, A.M.,Baron, R.A.,Wong, W., et al. A small-molecule inhibitor of isoprenylcysteine carboxyl methyltransferase with antitumor activity in cancer cells. Proceedings of the National Academy of Sciences of the United States of America 102(12), 4336-4341 (2005).
2.Baron, R.A.,Peterson, Y.K.,Otto, J.C., et al. Time-dependent inhibition of isoprenylcysteine carboxyl methyltransferase by indole-based small molecules. Biochemistry 46(2), 554-560 (2007).
3.Wang, M.,Tan, W.,Zhou, J., et al. A small molecule inhibitor of isoprenylcysteine carboxymethyltransferase induces autophagic cell death in PC3 prostate cancer cells. The Journal of Biological Chemisty 283(27), 18678-18684 (2008).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 376.5 |
| 分子式 | C25H32N2O |
| CAS号 | 851636-83-4 |
| 稳定性 | ≥ 1 year |
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