Bioactivity | NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (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[1]. |
Target | IC50: 38 nM (NNMT, in K562 cells), 42 nM (promega MTase-Glo methyltransferase assay) |
Invitro | 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 methyltransferase assay[1]. |
In Vivo | 1.19Pharmacokinetic Properties of NNMT-IN-4 in Mice[1]. |
Name | NNMT-IN-4 |
Formula | C9H11N3O |
Molar Mass | 177.20 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Barrows RD, et al. Potent Uncompetitive Inhibitors of Nicotinamide N-Methyltransferase (NNMT) as In Vivo Chemical Probes. J Med Chem. 2022 Nov 10;65(21):14642-14654. |