JBSNF-000028 TFA is an orally active nicotinamide N-metltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 TFA can be used for the research of metabolic disorders[1].
JBSNF-000028 TFA (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells[1].
JBSNF-000028 TFA (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells[1].
JBSNF-000028 TFA binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain)[1].
JBSNF-000028 TFA is inactive against a broad panel of targets related to metabolism and safety[1].
JBSNF-000028 TFA (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO)[1].
JBSNF-000028 TFA (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1].
[1]. Ruf S, et al. Novel tricyclic small molecule inhibitors of Nicotinamide N-metltransferase for the treatment of metabolic disorders. Sci Rep. 2022 Sep 14;12(1):15440.
















