Cas No.: | 1236188-16-1 |
Chemical Name: | 740 Y-P |
Synonyms: | 740 Y-P;740YPDGFR;PDGFR 740Y-P;PDGFR740Y-P;CID 90488730;RQIKIWFQNRRMKWKKSDGGYMDMS (Modifications: Tyr-21 = pTyr);740 Y-P, >96%;740 Y-P,740YPDGFR,PDGFR 740Y-P, >96%;L-Serine, L-arginyl-L-glutaminyl-L-isoleucyl-L-lysyl-L-isoleucyl-L-tryptophyl-L-phenylalanyl-L-glutaminyl-L-asparaginyl-L-arginyl-L-arginyl-L-methionyl-L-lysyl-L-tryptophyl-L-lysyl-L-lysyl-L-seryl-L-α-aspartylglycylglycyl-O-phosphono-L-tyrosyl-L-methionyl-L-α-aspartyl-L-methionyl-;740 Y-P (PDGFR 740Y-P);740 Y-P,740YPDGFR,PDGFR 740Y-P |
SMILES: | S(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])C([H])([H])C(N([H])C([H])([H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])O[H])=O)C([H])([H])C([H])([H])SC([H])([H])[H])=O)C([H])([H])C(=O)O[H])=O)C([H])([H])C([H])([H])SC([H])([H])[H])=O)C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OP(=O)(O[H])O[H])=O)=O)=O)C([H])([H])C(=O)O[H])=O)C([H])([H])O[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])C(N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C([H])([H])C(N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C([C@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C(N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])N([H])[H])=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O |
Formula: | C141H222N43O39PS3 |
M.Wt: | 3270.70 |
Purity: | 0.9 |
Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Description: | 740 Y-P (PDGFR 740Y-P) is a potent and cell permeable PI3K activator. |
Target: | PI3K |
In Vivo: | 740 Y-P is not only internalised in living cells but can also interact with p85 in vivo.[1] |
In Vitro: | 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]. |
Cell Assay: | 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]. |
References: | [1]. Derossi D, et al. Stimulation of mitogenesis by a cell-permeable PI 3-kinase binding peptide. |