GNE-617

• CAT Number: I001396
• CAS Number: 1362154-70-8
• Molecular Formula: C21H15F2N3O3S
• Molecular Weight: 427.426
• Purity: ≥95%
• Synonyms: N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide
• Target: NAMPT
• Solubility: 10 mM in DMSO
• Storage: Store at -20C
• IC50: 18.9 nM (in Hela) [1]
• IUPAC Name: N-[[4-(3,5-difluorophenyl)sulfonylphenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
• InChI: InChI=1S/C21H15F2N3O3S/c22-16-9-17(23)11-19(10-16)30(28,29)18-4-1-14(2-5-18)12-25-21(27)15-3-6-20-24-7-8-26(20)13-15/h1-11,13H,12H2,(H,25,27)
• InChIKey: XRDVXQQZLHVEQZ-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1CNC(=O)C2=CN3C=CN=C3C=C2)S(=O)(=O)C4=CC(=CC(=C4)F)F

GNE-617 (CAT: I001396) is a novel and specific inhibitor of nicotinamide phosphoribosyltransferase (Nampt). Nampt is an enzyme involved in the biosynthesis of nicotinamide adenine dinucleotide (NAD+), an essential coenzyme involved in various cellular processes, including energy metabolism and cell signaling. By inhibiting Nampt, GNE-617 disrupts the production of NAD+ and interferes with NAD+-dependent processes. This targeted inhibition of Nampt holds therapeutic potential in various diseases, including cancer, where NAD+ metabolism plays a critical role in tumor growth and survival.

Reference

[1]. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors.
[2]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Oct 4.