Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl-methanone
Purity: ≥98%
Formula Markup: C30H27BrN4O2
Formula Weight: 555.5
CAS Number: 226929-39-1
Notes: Farnesylation, the post-translational addition of a 15-carbon isoprenyl group, alters the function of several proteins, including Ras proteins.{21707,26419} 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.{27038} It displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I.{27038} 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.{27038} These effects are obtained both in RAW 264.7 mouse macrophages and in mice.{27038} LB42708 also inhibits Ras-dependent signaling in endothelial cells, stopping VEGF-mediated angiogenesis both in vitro and in vivo.{27039}
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