KRpep-2d peptide

KRpep-2d peptide

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

Batch to batch variation of the purity

Ac-RRRRCPLYISYDPVCRRRR-NH2, disulfide bridge between cysteines 5 and 15

Ac-Arg-Arg-Arg-Arg-Cys-Pro-Leu-Tyr-Ile-Ser-Tyr-Asp-Pro-Val-Cys-Arg-Arg-Arg-Arg-NH2

19

95.22%

C₁₀₈H₁₈₂N₄₄O₂₅S₂

2561

Synthetic

Powder

KRpep-2d is a potent K-Ras inhibitor, discovered after optimization of an initial hit obtained by phage display technology. KRpep-2d inhibits the enzyme activity of K-Ras(G12D) with an IC50 of 1.6 nM, and with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant in both cell-free enzyme and cell based assays. Mutated Ras proteins play important roles in cell differentiation, proliferation, and survival of various cancers, and K-Ras(G12D) is considered a very important target as K-Ras mutations underlie 86% of Ras-linked cancers, with 83% of K-Ras mutations being at the G12 residue. KRpep-2d can suppress ERK phosphorylation downstream of K-Ras(G12D) and reduce proliferation in A427 cancer 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

• Niida et al (2017) Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging. Bioorg Med Chem Lett. 27(12) 2757 PMID: 28457754
• Sakamoto et al (2017) K-Ras(G12D)-selective inhibitory peptides generated by random peptide T7 phage display technology. Biochem Biophys Res Commun. 484(3) 605 PMID: 28153726
• Lim et al (2021) Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling. Chem Sci. 12(48) 15975 PMID: 35024121

Trifluoroacetic acid (TFA) is a common counterion from the purification process using High-Performance Liquid Chromatography (HPLC). The presence of TFA can affect the peptide's net weight, appearance, and solubility.

Impact on Net Weight: The TFA salt contributes to the total mass of the product. In most cases, the peptide content constitutes >80% of the total weight, with TFA accounting for the remainder.

Solubility: TFA salts generally enhance the solubility of peptides in aqueous solutions.

In Biological Assays: For most standard in vitro assays, the residual TFA levels do not cause interference. However, for highly sensitive cellular or biochemical studies, please be aware of its presence.