產品描述: 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 |
靶點:
PI3K |
體外研究:
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 (HY-10108) or Wortmannin (HY-10197) 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. |
體內研究:
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 |
參考文獻:
1. Derossi D, et al. Stimulation of mitogenesis by a cell-permeable PI 3-kinase binding peptide. 2. Xiaoli Feng, et al. Graphene Oxide Induces p62/SQSTM-dependent Apoptosis Through the Impairment of Autophagic Flux and Lysosomal Dysfunction in PC12 Cells. Acta Biomater. 2018 Nov;81:278-292. 3. Zhiqing Sun, et al. GABAB Receptor-Mediated PI3K/Akt Signaling Pathway Alleviates Oxidative Stress and Neuronal Cell Injury in a Rat Model of Alzheimer's Disease. J Alzheimers Dis. 2020;76(4):1513-1526. |
溶解性:
Soluble in DMSO、H2O |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
0.306 ml |
1.529 ml |
3.057 ml |
5 mM |
0.061 ml |
0.306 ml |
0.611 ml |
10 mM |
0.031 ml |
0.153 ml |
0.306 ml |
50 mM |
0.006 ml |
0.031 ml |
0.061 ml |
|
注意: |
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