740 Y-P

740 Y-P (PDGFR 740Y-P) is a potent and cell permeable PI3K activator.

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

Research Areas >> Cancer

Peptides

Peptides

PI3K

740 Y-P is a synthetic biotinylated peptide consisting of the 16-amino acid sequence derived from the third helix of the Antennapedia protein in tandem with a 9 amino acid phosphopeptide mimetic of the high affinity p85 binding site on the PDGF receptor. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85. 740 Y-P fails to bind GST alone, or a GST fusion protein containing the N- terminal SH2 domain of PLCg and shows relatively weak binding of a GST fusion proteins containing the SH2 domain of Grb2. The 740 Y-P peptide is also able to specifically interact with p85 in cell lysates as shown by affinity precipitation. 740 Y-P stimulates mitogenesis at the lowest concentration tested (1 mg/mL). The peptide stimulates mitogenesis in both the presence and absence of serum (0.5%), and in the former instance a maximal response observed at 50 mg/mL. 740Y-P peptide to stimulate mitogenesis is highly specific and not a general feature of a cell permeable SH2 domain binding peptides[1].

740 Y-P is not only internalised in living cells but can also interact with p85 in vivo.[1]

Following serum starvation, C2 cells are cultured in the presence of the PDGFR 740Y-P peptide at the given concentrations (0, 1, 10, 100 μg/mL) for 48 h. The mitogenic response is assessed by measurement of the percentage of cells in S-phase[1].

[1]. Derossi D, et al. Stimulation of mitogenesis by a cell-permeable PI 3-kinase binding peptide.

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | LY3023414 | 1,3-Dicaffeoylquinic acid | GSK2126458(GSK458)