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Products
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- Resources
BM30
Cat. No. EI-010
Structure:
4-Hydroxyphenylacetyl-Pro-Lys-Arg-NH2
Activity:
N-terminal methyltransferase1/2 (NTMT1/2) inhibitor
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.
Mackie et al (2020) Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies. J Med Chem. 63(17) 9512 PMID: 32689795
Technical Data
| Structure | 4-Hydroxyphenylacetyl-Pro-Lys-Arg-NH2 |
| Molecular Weight | 532.64 |
| Formula | C25H40N8O5 |
| Sequence | XPKR-NH2 |
| Modifications | X is 4-hydroxyphenylacetyl, C terminal amide |
Solubility and Storage
| Solubility | Soluble in DMSO |
| Appearance | Freeze dried solid |
| Storage | Store desiccated, frozen and in the dark |
Batch Specific Data
| Purity | >95% by HPLC |
| Certificate of Analysis | EI-010-1MG BM30 CofA_66795827b0e52.pdf |
| Safety Data Sheet | BM30 MSDS_602ba9df144b8.pdf |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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