Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).
ターゲット&IC50 | FTase (H-ras):0.8 nM, FTase (K-Ras):2.0 nM, FTase (N-ras):1.2 nM |
In vitro | In mice treated with lipopolysaccharide (LPS), LB42708 (12.5 mg/kg, intraperitoneally) inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β), and suppressed the progression of collagen-induced arthritis (CIA). Additionally, in tumors with either wild-type or mutated Ras, LB42708 (20 mg/kg/day, intraperitoneally) inhibited tumor growth and angiogenesis. |
In vivo | LB42708 exerts an irreversible inhibitory effect on growth and induces apoptosis in rat intestinal epithelial cells altered by H-ras and K-ras. It inhibits VEGF-induced tumor angiogenesis in tumor-associated endothelial cells by blocking the Ras-dependent MAPK and PI3K/Akt signaling pathways. Additionally, in the murine macrophage lineage RAW264.7 cells, LB42708 significantly inhibits the process of lipopolysaccharide + IFN-γ induced intracellular farnesylation of the protein p21ras. In immune-activated osteoblasts and macrophages, LB42708 suppresses the production of nitric oxide synthase, cyclooxygenase-2, TNF-α, IL-1β, NO, and PGE(2). By inhibiting IKK activity, LB42708 also represses the activation of NF-κB and the activity of the iNOS promoter. |
分子量 | 555.47 |
分子式 | C30H27BrN4O2 |
CAS No. | 226929-39-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 55.6 mg/mL (100 mM)
DMSO: 55.6 mg/mL (100 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LB42708 226929-39-1 Metabolism Transferase Ftase Apoptosis Inhibitor H-Ras orally active K-Ras4B N-Ras Farnesyl Transferase inhibit LB-42708 farnesyltransferase inhibitor LB 42708 inhibitor