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Submit ReviewLB 42708
Description: Selective farnesyltransferase (FTase) inhibitor
Chemical Name: [1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone
Purity: ≥98% (HPLC)
Biological Activity 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.
Technical Data for LB 42708
| M. Wt | 555.46 |
| Formula | C30H27BrN4O2 |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for LB 42708
References for LB 42708
References are publications that support the biological activity of the product.
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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Keywords: LB 42708, LB 42708 supplier, LB42708, ftase, farnesyltransferase, inhibitors, inhibits, selective, Protein, Prenyltransferases, Post-translational, Modifications, 4294, Tocris Bioscience
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