Novel peptidomimetic probes for NTMT1/2

Protein N-terminal methyltransferases (NTMTs) methylate the α-N-terminal amines of proteins starting with the canonical X-P-K/R motif.  Genetic studies imply that NTMT1 regulates cell mitosis and DNA damage repair.  Isca Biochemicals are pleased to announce the availability of first potent peptidomimetic inhibitors for NTMT1/2, BM30, a competitive inhibitor to the peptide substrate but noncompetitive to the cofactor S-adenosylmethionine, and the analogue DC432 which is BM30 made cell permeable by the addition of five arginine residues.  BM30 exhibits over 100-fold selectivity to NTMT1/2 among a panel of 41 MTs, suggesting the potential for high selectivity when targeting the peptide substrate binding site of NTMT1/2. The cell-permeable analogue DC432 (IC50 of 54 ± 4 nM) decreases the N-terminal methylation level of the regulator of chromosome condensation 1 and SET proteins in HCT116 cells.  These peptides are valuable probes for NTMT1/2 and will allow the opportunity to help elucidate the function of NTMTs in the future.  Place an order for either peptide from before the end of October and receive a 10% discount (please quote NTNM 1020 when placing an order)