Human PD-L1 inhibitor Ar5Y_4 peptide

Human PD-L1 inhibitor Ar5Y_4 peptide

• COA/MS/HPLC Report
• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

GNWDYNSQRAQLYNQ

H-Gly-Asn-Trp-Asp-Tyr-Asn-Ser-Gln-Arg-Ala-Gln-Leu-Tyr-Asn-Gln-OH

15

98.62%

C₈₀H₁₁₃N₂₅O₂₇

1856.89

Synthetic

Powder

Blocking the interaction of human programmed death 1 (hPD-1) and its ligand hPD-L1 has been a promising immunotherapy in cancer treatment. Human PD-L1 inhibitor (Ar5Y_4, GNWDYNSQRAQLYNQ) showed a KD value of 1.38 ± 0.39 μM, comparable to the binding affinity of the cognate hPD-L1. A Surface Plasmon Resonance (SPR) competitive binding assay result indicated that Ar5Y_4 could inhibit the interaction of hPD-1/hPD-L1. Moreover, Ar5Y_4 could restore the function of Jurkat T cells which had been suppressed by stimulated HCT116 cells. Human PD-L1 inhibitor provides promising biologic candidates for cancer immunotherapy or diagnostics.

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

• Li Q, Quan L, Lyu J, et al. Discovery of peptide inhibitors targeting human programmed death 1 (PD-1) receptor. Oncotarget. 2016;7(40):64967-64976

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.