NNMT Inhibitor Screening Assay Kit

N′-Nicotinamide Methyltransferase (NNMT) (E.C. 2.1.1.1) catalyzes the N-methylation of nicotinamide, pyridines, and other analogues using S-adenosyl methionine (SAM) as the donor resulting in the production of 1-methylnicotinamide (MNA). NNMT plays a significant role in the regulation of metabolic pathways and is expressed at markedly high levels in several kinds of cancers, neurodegenerative diseases, obesity and diabetes, indicating it is a potential molecular target for therapy.

Suitable for screening/studying/characterizing potential inhibitors of N′-Nicotinamide Methyltransferase (NNMT).

This NNMT inhibitor screening kit utilizes SAM as the methyl group donor and nicotinamide as the substrate. NNMT methylates nicotinamide generating S-adenosylhomocysteine (SAH) and 1-methylnicotinamide. The SAH is hydrolyzed by SAH hydrolase to form homocysteine, the free thiol group of which is detected using the Thiol Detecting Probe, generating an enhanced fluorescence signal (λex = 392 nm/ λem = 482 nm). In the presence of an NNMT inhibitor, the enzymatic activity is inhibited resulting in decreased fluorescence. This assay kit is a simple, sensitive, and rapid tool to screen potential inhibitors of NNMT.