NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-metltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 38 nM in K562 cells[1].NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 42 nM in promega MTase-Glo metltransferase assay[1].
1.19Pharmacokinetic Properties of NNMT-IN-4 in Mice[1].
References:
[1]. Barrows RD, et al. Potent Uncompetitive Inhibitors of Nicotinamide N-Metltransferase (NNMT) as In Vivo Chemical Probes. J Med Chem. 2022 Nov 10;65(21):14642-14654.