PKI (14-22) amide, myristoylated peptide

PKI (14-22) amide, myristoylated peptide

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

Myrisitic Acid-GRTGRRNAI-NH2

Myrisitic Acid-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-NH2

9

95.76%

C₅₃H₁₀₀N₂₀O₁₂

1209.48

Synthetic

Powder

PKI (14 - 22) amide, myristoylated, is a cell-permeable version of the protein kinase inhibitor (PKI) PKI (14-22) amide. When non-myristoylated, PKI (14-22) amide inhibits protein kinase A with a Ki of 36 nM and also inhibits cell growth and induces apoptosis in human pancreatic cancer cells (PANC-1). Myristoylated peptides as a class may exhibit off-target activation of the funny current If in sinoatrial myocytes.

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

• Glass et al (1989) Primary structural determinants essential for potent inhibition of cAMP-dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitory protein. J.Biol.Chem. 264 8802 PMID: 2722799
• Farrow et al (2003) Inhibition of pancreatic cancer cell growth and induction of apoptosis with novel therapies directed against protein kinase A. Surgery 134 197 PMID: 12947318
• Liao et al (2011) Myristoylated peptides potentiate the funny current I(f) in sinoatrial myocytes. Channels 5(2) 115 doi:10.4161/chan.5.2.14195

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.