Molecular Weight(MW): 555.46
LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.
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Choose Selective Transferase Inhibitors
|Description||LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.|
LB42708 potently inhibits the processing of the cellular farnesylated protein p21ras induced by LPS + IFN-γ in murine macrophage cell line RAW264.7 cells. LB42708 inhibits NF-κB activation and iNOS promoter activity through the inhibition of IKK activity. Moreover, LB42708 suppresses the expression of inducible NO synthase, cyclooxygenase-2, TNF-alpha, and IL-1beta and the production of NO and PGE(2) in immune-activated macrophages and osteoblasts.  LB42708 irreversibly inhibits growth and induces apoptosis in H-ras and K-ras-transformed rat intestinal epithelial cells.  LB42708 inhibits of VEGF-induced tumor angiogenesis by blocking Ras-dependent MAPK and PI3K/Akt pathways in tumor-associated endothelial cells. 
|In vivo||LB42708 (12.5 mg/kg i.p.) inhibits production of NO, PGE2, TNF-α, and IL-1β in LPS-injected mice, and also prevents the development of CIA.  LB42708 (20 mg/kg/day i.p.) also inhibits tumor growth and angiogenesis in both Ras wild-type and mutated tumors. |
|In vitro||DMSO||100 mg/mL (180.03 mM)|
|Ethanol||86 mg/mL warmed (154.82 mM)|
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