Biochem/physiol Actions

5-Amino-1-methylquinolinium (5-amino-1MQ) is a substrate site-targeting, selective nicotinamide N-methyltransferase (NNMT) inhibitor (IC₅₀ = 1.2 μM; 50 μM SAM, 100 μM NCA) that reduces 3T3-L1 lipogenesis (EC₅₀ = 30μM) and adipocytes 1-methylnicotinamide level (EC₅₀ = 2.3 μM) without affecting related methyltransferases & enzymes in the NAD+ salvage pathway. 5-amino-1MQ shows in vivo therapeutic efficacy in murine models of DIO (20 mg/kg/d sc.), muscle injury (5 or 10 mg/kg bid. sc.), and intraperitoneal HeyA8 ovarian cancer metastasis (20 mg/kg/d ip.) with no adverse effects to the animals (up to 60 mg/kg/d). Note:1.89 mg iodide salt contains 1 mg eq of 5-amino-1MQ.