DC432 peptide

DC432 peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

XPKRRRRRR-NH2, X is 4-hydroxyphenylacetyl

9

95.5%

C₅₅H₁₀₀N₂₈O₁₀

1313.59

Synthetic

Powder

DC432 is a cell permeable analogue of BM30, also available, the first potent peptidomimetic substrate competitive inhibitor of N-terminal methyltransferase1/2 (NTMT1/2), one of a family of enzymes which methylate the α-N-terminal amines of proteins starting with the canonical X-P-K/R motif. DC432 has been made cell permeable by the addition of five arginine residues to BM30. DC432 decreases the N-terminal methylation level of the regulator of chromosome condensation 1 and SET proteins in HCT116 cells.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Mackie et al (2020) Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies. J Med Chem. 63(17) 9512 doi:10.1021/acs.jmedchem.0c00689

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.