LB 42708

Cat. No. 4294

LB 42708 C30H27BrN4O2 [226929-39-1]

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Chemical Name: [1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone

Biological Activity

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

M.Wt:
555.46
Formula:
C30H27BrN4O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
226929-39-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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Keywords: LB 42708, supplier, LB42708, ftase, farnesyltransferase, inhibitors, inhibits, selective, Tocris Bioscience, Protein Prenyltransferase Inhibitor products

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