N-(4-((3-(trifluoromethyl)phenyl)sulfonyl)benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide

Description

GNE-618 is an inhibitor of nicotinamide phosphoribosyl transferase (NAMPT).

Uses

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity[1].

in vivo

References

[1] Xiao Y, et al. Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway rendersthem sensitive to NAMPT inhibition with GNE-618. Neoplasia. 2013 Oct;15(10):1151-60. DOI:10.1593/neo.131304
[2] XIAOZHANG ZHENG . Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23 20: Pages 5488-5497. DOI: 10.1016/j.bmcl.2013.08.074