LB 42708

Farnesylation, the post-translational addition of a 15-carbon isoprenyl group, alters the function of several proteins, including Ras proteins. 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. It displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I. LB 42708 prevents the farnesylation of H-Ras in response to LPS plus IFN-gamma (IC50 = 10 nM), preventing activation of NF-kappaB as well as downstream signaling. These effects are obtained both in RAW 264.7 mouse macrophages and in mice. LB42708 also inhibits Ras-dependent signaling in endothelial cells, stopping VEGF-mediated angiogenesis both in vitro and in vivo.Formal Name: [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl-methanone. CAS Number: 226929-39-1. Molecular Formula: C30H27BrN4O2. Formula Weight: 555.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:5): 0.1 mg/ml. lambdamax: 223, 296 nm. SMILES: O=C(C1=CN(CC2=CN=CN2CC3=CC=C(Br)C=C3)C=C1C4=CC=CC5=C4C=CC=C5)N6CCOCC6. InChi Code: InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2. InChi Key: GUUIRIMAQGOLHT-UHFFFAOYSA-N.