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Submit ReviewLB 42708
说明： Selective farnesyltransferase (FTase) inhibitor
化学名： [1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone
纯度： ≥98% (HPLC)
生物活性 for LB 42708
Selective inhibitor of farnesyltransferase (FTase). Blocks farnesylation of H-Ras, N-Ras and K-Ras4B (IC50 values are 0.8, 1.2 and 2.0 nM respectively). Displays >50,000-fold selectivity for FTase over geranylgeranyltransferase (GGTase) I. Inhibits VEGF-induced Ras activation; suppresses angiogenesis in vivo and in vitro (IC50 = 75 nM). Orally active.
技术数据 for LB 42708
| 分子量 | 555.46 |
| 公式 | C30H27BrN4O2 |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 226929-39-1 |
| PubChem ID | 10099206 |
| InChI Key | GUUIRIMAQGOLHT-UHFFFAOYSA-N |
| Smiles | O=C(N4CCOCC4)C1=CN(CC5=CN=CN5CC6=CC=C(Br)C=C6)C=C1C2=CC=CC3=C2C=CC=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for LB 42708
参考文献 for LB 42708
参考文献是支持产品生物活性的出版物。
Na et al (2004) Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppresion of p21ras-dependent NF-κB activation. J.Immunol. 173 1276 PMID: 15240720
Kim et al (2010) 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. Mol.Pharmacol. 78 142 PMID: 20406854
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关键词: LB 42708, LB 42708 supplier, LB42708, ftase, farnesyltransferase, inhibitors, inhibits, selective, Protein, Prenyltransferases, Post-translational, Modifications, 4294, Tocris Bioscience
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