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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-LB42708
LB42708

Chemical Structure : LB42708

CAS No.: 226929-39-1

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LB42708 (LB-42708)

货号: PC-26365Not For Human Use, Lab Use Only.

LB42708 (LB-42708) is a potent, selective and orally active farnesyltransferase (FTase) inhibitor, inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50 values of 0.8 nM, 1.2 nM and 2.0 nM, respectively, inhibits p21(ras)-dependent NF-kappaB activation.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LB42708 (LB-42708) is a potent, selective and orally active farnesyltransferase (FTase) inhibitor, inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50 values of 0.8 nM, 1.2 nM and 2.0 nM, respectively, inhibits p21(ras)-dependent NF-kappaB activation.
LB42708 suppressed NF-kappaB activation and iNOS promoter activity by suppressing the I-kappaB kinase activity and I-kappaBalpha degradation.
LB42708 significantly decreased the incidence and severity of arthritis as well as mRNA expression of inducible NO synthase, cyclooxygenase-2, TNF-alpha, and IL-1beta in the paws of collagen-induced arthritic mice.
LB42708 inhibited VEGF-induced Ras activation and subsequently suppressed angiogenesis in vitro and in vivo by blocking the mitogen-activated protein kinase kinase/extracellular signal-regulated kinase/p38 mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K)/Akt/endothelial nitric-oxide synthase pathways in endothelial cells without altering FAK/Src activation.
LB42708 suppressed tumor growth and tumor angiogenesis in both xenograft tumor models of Ras-mutated HCT116 cells and its wild-type Caco-2 cells.

物理化学性质&存储条件

分子量 555.48
分子式 C30H27BrN4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(1-((1-(4-Bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

参考文献

1. Hee-Jun Na, et al. J Immunol. 2004 Jul 15;173(2):1276-83.

2. Kim CK, et al. Mol Pharmacol. 2010 Jul;78(1):142-50.

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