MS2734 is a novel Bisubstrate Inhibitor of Nicotinamide N-Methyltransferase (NNMT). MS2734 inhibited the hNNMT methyltransferase activity with an IC50 of 14 ± 1.5 μM. MS2734 was a tight binding ligand for hNNMT using ITC (Kd = 2.7 ± 0.2 μM). In MOA studies, MS2734 was competitive with the cofactor SAM and noncompetitive with the substrate nicotinamide. The crystal structure of human NNMT in complex with MS2734 has clearly demonstrated that MS2734 occupied both substrate and cofactor binding sites.
MedKoo Cat#: 533700
Name: MS-2734
CAS#: 2587612-25-5
Chemical Formula: C24H32N8O6
Exact Mass: 528.2445
Molecular Weight: 528.57
Elemental Analysis: C, 54.54; H, 6.10; N, 21.20; O, 18.16
The following data is based on the product molecular weight 528.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
