MN58b

MN58b is a first-generation, selective small molecule inhibitor of choline kinase alpha (ChoKα), an enzyme that catalyzes the phosphorylation of choline to phosphocholine in the Kennedy pathway for phosphatidylcholine biosynthesis. Developed by the Spanish National Research Council (CSIC), Universidad Autónoma de Madrid, and TCD Pharma, MN58b has been widely utilized as a preclinical research tool to study the therapeutic potential of ChoKα inhibition in oncology and inflammatory diseases. By blocking ChoKα, MN58b disrupts cancer cell lipid metabolism, leading to decreased phosphocholine levels, cell cycle arrest in normal cells, and the induction of apoptosis in tumor cells. Preclinical studies have demonstrated its efficacy in various cancer models, including breast, lung, colorectal, bladder, and pancreatic cancers, as well as in models of rheumatoid arthritis and malaria. Although MN58b itself did not advance to clinical trials due to a narrow therapeutic window, it served as the lead compound for the development of second-generation clinical candidates such as TCD-717 (RSM-932A).

Other names

1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide1,4-[4-4′-Bis-{[4-(dimethylamine)pyridinium-1-yl]methyl}diphenyl]butane dibromideMN58b bromideMN-58b bromideMN 58b bromide