[CAS NO. 226929-39-1] LB42708

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PRODUCTS SPECIFICATIONS [226929-39-1]

Catalog

SLK-S7467

Brand

Selleck

CAS

226929-39-1

DESCRIPTION [226929-39-1]

Overview

MDL	-
Molecular Weight	555.46
Molecular Formula	C30H27BrN4O2
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8003 mL	9.0015 mL	18.0031 mL
5 mM	0.3601 mL	1.8003 mL	3.6006 mL
10 mM	0.1800 mL	0.9002 mL	1.8003 mL
50 mM	0.0360 mL	0.1800 mL	0.3601 mL

Description

LB42708 is an orally active inhibitor with of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.

Targets

FTase (H-ras) ^[1]	FTase (N-ras) ^[1]	FTase (K-Ras) ^[1]
0.8 nM	1.2 nM	2.0 nM

In vitro

LB42708 potently inhibits the processing of the cellular farnesylated protein p21 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.

References

[1] Na HJ, et al. J Immunol. 2004, 173(2), 1276-1283.
[2] Kim HS, et al. Toxicol Appl Pharmacol. 2006, 215(3), 317-329.
[3] Kim CK, et al. Mol Pharmacol. 2010, 78(1), 142-150