| 货号 | 16428-1mg |
| 描述 | Farnesylation, the post-translational addition of a 15-carbon isoprenyl group, alters the function of several proteins, including Ras proteins.1,2 LB 42708 is a potent inhibitor of farnesyltransferase (FTase), blocking farnesylation of H-Ras, N-Ras, and K-Ras4B with IC50 values of 0.8, 1.2, and 2.0 nM, respectively.3 It displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I.3 LB 42708 prevents the farnesylation of H-Ras in response to LPS plus IFN-γ (IC50 = 10 nM), preventing activation of NF-κB as well as downstream signaling.3 These effects are obtained both in RAW 264.7 mouse macrophages and in mice.3 LB42708 also inhibits Ras-dependent signaling in endothelial cells, stopping VEGF-mediated angiogenesis both in vitroandin vivo.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Appels, N.M.G.M.,Beijnen, J.H. and Schellens, J.H.M. Development of farnesyl transferase inhibitors: A review. Oncologist 10, 565-578 (2005). 2.Berndt, N.,Hamilton, A.D. and Sebti, S.M. Targeting protein prenylation for cancer therapy. Nature Reviews.Cancer 11(11), 775-791 (2011). 3.Na, H.J.,Lee, S.J.,Kang, Y.C., et al. Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21ras-dependent NF-κB activation. Journal of Immunology 173(2), 1276-1283 (2004). 4.Kim, C.K.,Choi, Y.K.,Ha, K.S., et al. The farnesyltransferase inhibitor LB42708 suppresses vascular endothelial growth factor-induced angiogenesis by inhibiting ras-dependent mitogen-activated protein kinase and phosphatidylinositol 3-kinase/Akt signal pathways. Molecular Pharmacology 78(1), 142-150 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 555.5 |
| 分子式 | C30H27BrN4O2 |
| CAS号 | 226929-39-1 |
| 稳定性 | ≥ 2 years |
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