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LB 42708
Axon 1794
CAS:
226929-39-1
Purity:
99%
- Soluble in DMSO
- MF: C30H27BrN4O2
- MW: 555.46
Description
LB 42708 is a selective, orally available farnesyltransferase (FTase) inhibitor with reported IC50 values of 0.8 nM in vitro and 8 nM in cells for inhibition of p21-Ras farnesylation.
Farnesyltransferase catalyzes lipid modification of Ras and other signaling proteins, enabling membrane localization and oncogenic pathway activation. LB 42708 is useful for studying prenylation-dependent signal transduction and Ras-associated cancer biology.
Key Features
- Potent FTase inhibitor
- IC50: 0.8 nM in vitro and 8 nM in cellular p21-Ras farnesylation assays
- Blocks farnesylation-dependent Ras membrane targeting
- Orally available tool for prenylation pathway research
Applications
- Protein prenylation and FTase enzyme studies
- Ras localization and MAPK pathway research
- Oncology signaling and antiproliferative assays
- Cellular farnesylation assay development
More Information
| Parent CAS No. | 226929-39-1 |
|---|---|
| Chemical Name | (1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone |
| SMILES | C(C1C(C2=C3C(C=CC=C3)=CC=C2)=CN(CC2N(CC3=CC=C(Br)C=C3)C=NC=2)C=1)(N1CCOCC1)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2 |
| InChiKey | GUUIRIMAQGOLHT-UHFFFAOYSA-N |
| CID | 10099206 |
| Short Description | FTase inhibitor |
LB 42708
potent FTase inhibitor
LB42708
Farnesyltransferase
FTase
Inhibitor
MAPK/ERK signaling
Protein prenylation and FTase enzyme studies
Ras localization and MAPK pathway research
Oncology signaling and antiproliferative assays
Cellular farnesylation assay development
cancer biology
receptor selectivity
signal transduction
enzyme pharmacology
drug discovery
CAS 226929-39-1
Axon Medchem
Axon 1794
Supplier
Vendor
References
- HJ Na et al. Inhibition of Farnesyltransferase Prevents Collagen-Induced Arthritis by Down-Regulation of Inflammatory Gene Expression through Suppression of p21ras-Dependent NF-κB Activation. J. Immunol. 2004, 173, 1276-1283.
- CK Kim et al. The farnesyltransferase inhibitor LB42708 suppresses vascular endothelial growth factor-induced angiogenesis by inhibiting Ras-dependent mitogen-activated protein kinase and PI3K/Akt signal pathways. Mol. Pharmacol. 2010, 78, 142-150.
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