A potent inhibitor of FTase

LB 42708 – 5 mg

Brand:
Cayman
CAS:
226929-39-1
Storage:
-20
UN-No:
Non-Hazardous - /

Farnesylation, the post-translational addition of a 15-carbon isoprenyl group, alters the function of several proteins, including Ras proteins.{21707,26419} LB 42708 is a potent inhibitor of farnesyltransferase (FTase), blocking farnesylation of H-Ras, N-Ras, and K-Ras4B with IC50 values of 0.8, 1.2, and 2.0 nM, respectively.{27038} It displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I.{27038} LB 42708 prevents the farnesylation of H-Ras in response to LPS plus IFN-γ (IC50 = 10 nM), preventing activation of NF-κB as well as downstream signaling.{27038} These effects are obtained both in RAW 264.7 mouse macrophages and in mice.{27038} LB42708 also inhibits Ras-dependent signaling in endothelial cells, stopping VEGF-mediated angiogenesis both in vitro and in vivo.{27039}  

 

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Description

A potent inhibitor of FTase, blocking farnesylation of H-Ras, N-Ras, and K-Ras4B with IC50 values of 0.8, 1.2, and 2.0 nM, respectively; displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I

Formal name: [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl-methanone

Synonyms: 

Molecular weight: 555.5

CAS: 226929-39-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Immunology & Inflammation|Innate Immunity

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