Rad17 derived peptide

Rad17 derived peptide

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

Batch to batch variation of the purity

H-ASELPASQPQPFSAKKK-OH

H-Ala-Ser-Glu-Leu-Pro-Ala-Ser-Gln-Pro-Gln-Pro-Phe-Ser-Ala-Lys-Lys-Lys-OH

17

95.69%

C₈₁H₁₃₂N₂₂O₂₅

1814.04

Synthetic

Powder

Rad17 derived peptide is an ATR (ATM and Rad-3) related kinase substrate. ATR is a serine/threonine-specific protein kinase that along with ATM (ataxia telangiectasia mutated) is involved in sensing DNA damage and activating the DNA damage checkpoint, leading to cell cycle arrest. ATR inhibition sensitises cancer cells to DNA damaging agents, making it an attractive target for cancer therapy. Rad17 derived peptide is an effective substrate in ATR kinase assays and has been used succesfully to identify novel ATR kinase inhibitors.

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

• Kim et al (1999) Substrate specificities and identification of putative substrates of ATM kinase family members. J Biol Chem. 274(53) 37538 PMID: 10608806
• Charrier et al (2011) Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. J Med Chem. 54(7) 2320 PMID: 21413798
• Kawasumi et al (2014) Identification of ATR-Chk1 pathway inhibitors that selectively target p53-deficient cells without directly suppressing ATR catalytic activity. Cancer Res. 74(24) 7534 PMID: 25336189

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.