226929-39-1

226929-39-1 structure

Name: LB 42708
Chemical Name: [1-{[1-(4-Bromobenzyl)-1H-imidazol-5-yl]methyl}-4-(1-naphthyl)-1H -pyrrol-3-yl](4-morpholinyl)methanone
CAS Number: 226929-39-1
Molecular Formula: C₃₀H₂₇BrN₄O₂
Molecular Weight: 555.465
Catalog: Biochemical Inhibitor Metabolism Transferase inhibitor
Create Date: 2016-12-09 16:53:45
Modify Date: 2024-01-13 19:18:53
LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively[1].

Name	[1-{[1-(4-Bromobenzyl)-1H-imidazol-5-yl]methyl}-4-(1-naphthyl)-1H -pyrrol-3-yl](4-morpholinyl)methanone
Synonyms	[1-{[1-(4-Bromobenzyl)-1H-imidazol-5-yl]methyl}-4-(1-naphthyl)-1H-pyrrol-3-yl](4-morpholinyl)methanone Methanone, [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl- LB42708

Description	LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Inflammation/Immunology Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase
In Vitro	LB42708 induces cell death despite K-ras prenylation. Growth inhibition by LB42708 is accompanied by G1 and G2/M cell cycle arrests in H-ras and K-ras-transformed RIE cells, respectively. LB42708 induces the upregulation of p21(CIP1/WAF1) and RhoB above the basal level that leads to the cell cycle arrest and to distinct morphological alterations of ras-transformed rat intestinal epithelial (RIE) cells[2].
References	[1]. Hee-Jun Na, et al. Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation. J Immunol. 2004 Jul 15;173(2):1276-83. [2]. Han-Soo Kim, et al. The farnesyltransferase inhibitor, LB42708, inhibits growth and induces apoptosis irreversibly in H-ras and K-ras-transformed rat intestinal epithelial cells. Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29.