| 货号 | 16176-5mg |
| 描述 | Post-translational protein prenylation, a process catalyzed by three different enzymes, occurs at the C-terminal of a number of proteins involved in cell growth control and oncogenesis. One of these enzymes, geranylgeranyltransferase I (GGTase I) modifies cysteines of proteins with CAAX terminal sequences, preferring either leucine or isoleucine in the X-position. The Rho family of proteins are typically geranylgeranylated by GGTase I.1 GGTI 298 is a CAAX peptidomimetic that selectively inhibits GGTase I with little effect on other prenylation enzymes such as farnesyltransferase.2 It has been shown to arrest human tumor cells (IC50 = 10 µM for A549 cells) in G0/G1 and induce apoptosis by inhibiting proteasome activity and up-regulating the expression of the cyclin-dependent kinase inhibitor p21.2,3,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Li, X.,Liu, L.,Tupper, J.C., et al. Inhibition of protein geranylgeranylation and RhoA/RhoA kinase pathway induces apoptosis in human endothelial cells. The Journal of Biological Chemisty 277(18), 15309-15316 (2002). 2.Miquel, K.,Pradines, A.,Sun, J., et al. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. Cancer Research 57, 1846-1850 (1997). 3.Efuet, E.T. and Keyomarsi, K. Farnesyl and geranylgeranyl transferase inhibitors induce G1 arrest by targeting the proteasome. Cancer Research 66(2), 1040-1051 (2006). 4.Vogt, A.,Sun, J.,Qian, Y., et al. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21WAF1/CIP1/SDI1 in a p53-independent manner. The Journal of Biological Chemisty 272(43), 27224-27229 (1997). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 593.7 |
| 分子式 | C27H33N3O3S • CF3COOH |
| CAS号 | 1217457-86-7 |
| 稳定性 | ≥ 2 years |
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