740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
IC50&Target
PI3K
体外研究
740 Y-P (50 μg/mL; 48 hours) specificly stimulates mitogenesis in medium is better than EGF or FGF at stimulating entry into S-phase, it shows the percentage of cells in S-phase for 48.3% in C2 cells. Additionally, LY294002 or Wortmannin potently inhibits the mitogenic response stimulated by the peptide. 740 Y-P (1 μg/mL) stimulates mitogenesis at the lowest concentration tested. 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 μg/mL. 740Y-P to stimulate mitogenesis is highly specific and not a general feature of a cell permeable SH2 domain binding peptides. 740 Y-P (30 μM; 24 hours) remarkably inhibits the level of LC3-II/LC3-I in GO-induced PC12 cells.
Western Blot Analysis
Cell Line:
PC12 cells
Concentration:
30 μM
Incubation Time:
24 hours
Result:
Inhibited the protein expression of LC3-II.
体内研究
740 Y-P is not only internalised in living cells but can also interact with p85 in vivo. 740 Y-P (intraperitoneal injection; 10 mg/kg; 6 weeks) decreases the degree of ROS levels in Aβ(25-32) treated hippocampal tissues and increases the extent of AKT and PI3K phosphorylation in alzheimer’s disease (AD) rat model.
分子式
C141H222N43O39PS3
分子量
2272.61
CAS号
1236188-16-1
运输条件
Room temperature in continental US; may vary elsewhere.