740 Y-P(Synonyms: 740YPDGFR; PDGFR 740Y-P)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

740 Y-P (Synonyms: 740YPDGFR; PDGFR 740Y-P) 纯度: 98.85%

740 Y-P (740YPDGFR; PDGFR 740Y-P) 是一个有效的,具有细胞渗透性的 PI3K 激活剂。740 Y-P 很容易结合含有 p85 的 N- 和 C- 末端 SH2 结构域的 GST 融合蛋白,但不能单独结合 GST。

740 Y-P(Synonyms: 740YPDGFR;  PDGFR 740Y-P)

740 Y-P Chemical Structure

CAS No. : 1236188-16-1

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1 mg ¥1000 In-stock
5 mg ¥2800 In-stock
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50 mg   询价  

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生物活性

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[1].

IC50 & Target[1]

PI3K

 

体外研究
(In Vitro)

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[1].
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[1].
740 Y-P (30 μM; 24 hours) remarkably inhibits the level of LC3-II/LC3-I in GO-induced PC12 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: PC12 cells
Concentration: 30 μM
Incubation Time: 24 hours
Result: Inhibited the protein expression of LC3-II.

体内研究
(In Vivo)

740 Y-P is not only internalised in living cells but can also interact with p85 in vivo[1].
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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

3270.70

Formula

C141H222N43O39PS3

CAS 号

1236188-16-1

Sequence Shortening

RQIKIWFQNRRMKWKKSDGG-{PO2Y}-MDMS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL (7.64 mM; Need ultrasonic)

H2O : 2 mg/mL (0.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3057 mL 1.5287 mL 3.0574 mL
5 mM 0.0611 mL 0.3057 mL 0.6115 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

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