BM30 is the first potent peptidomimetic inhibitor for N-terminal methyltransferase1/2 (NTMT1/2). BM30 has a half-maximal inhibitory concentration of 0.89 0.10 µM, is a competitive inhibitor to the peptide substrate and is noncompetitive to the cofactor S-adenosylmethionine. BM30 exhibits over 100-fold selectivity for NTMT1/2 among a panel of 41 methyl transferases, showing great potential for high selectivity when targeting the peptide substrate binding site of NTMT1/2. Its cell-permeable analogue DC432 is also available, which can decrease the N-terminal methylation level of the regulator of chromosome condensation 1 and SET proteins in HCT116 cells.
