2. PI3K/Akt/mTOR
  3. PDK-1
  4. PS48

PS48 是 一种 PDK1 激活剂，AC50 为 8 μM。

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PS48 Chemical Structure

PS48 Chemical Structure

CAS No. : 1180676-32-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥800
In-stock
25 mg ￥1500
In-stock
50 mg ￥2200
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

PS48 相关抗体

Top Publications Citing Use of Products

    PS48 purchased from MCE. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275.  [Abstract]

    Suppression of PDK1/Akt/mTOR pathway by TP in HG-treated HRMCs was also reversed by PS48.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PS48 is an activator of PDK1 with an AC50 of 8 μM.

    IC50 & Target

    AC50: 8 μM (PDK1)[1]
    体外研究
    (In Vitro)

    PS48 activates full length PDK1 (His-PDK1- FL) and PDK1 50-359[Tyr288Gly;Gln292Ala] (His-PDK1 dm) with AC50s (the concentrations required to reach 50% of the maximal activation) of 7.95±0.2 and 10.0±2.0 μM, respectively. PS48 binds to PDK150–359 with a 1:1 stoichiometry and a binding affinity in the micromolar range (Kd=10.3 μM)[1]. PDK1 activator, PS48, has the ability to reverse the cell proliferation inhibition role of triptolide (TP) in vitro. The inhibition role of TP in cell number is significantly reversed by PS48. TP significantly increases the cell proportion in G0-G1 phase and decreases the cell proportion in G2-M and S phase. However, the effect of TP on cell cycle distribution is all reversed by PS48. In addition, suppression of PDK1/Akt/mTOR pathway by TP in high glucose (HG)-treated human renal mesangial cells (HRMCs) is also reversed by PS48, as well as the expression of Ki-67 and proliferating cell nuclear antigen (PCNA)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    PS48 相关抗体:
    分子量

    286.75

    Formula

    C17H15ClO2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (348.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.4874 mL 17.4368 mL 34.8736 mL
    5 mM 0.6975 mL 3.4874 mL 6.9747 mL
    查看完整储备液配制表

    * 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。-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。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

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

      Solubility: ≥ 2.5 mg/mL (8.72 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (8.72 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（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。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [1]

    PDK1 activity tests are performed using T308tide as a substrate for PDK1. In brief, PDK1 activity assay is performed at room temperature (22°C) in a 20 μL mix containing 50 mM Tris pH 7.5, 0.05 mg/mL BSA, 0.1% β-mercaptoethanol, 10 mM MgCl2, 100 μM [γ32P]ATP (5-50 cpm/pmol) , 0.003% Brij, 150-500 ng PDK1, and T308tide (from 0.1 to 1 mM). When appropriate, the PDK1 activity assay is performed in a 96 well format and 4 μL aliquots spotted on p81 phosphocellulose papers using ep motion 5070, washed in 0.01% phosphoric acid, dried, and then exposed and analysed using PhosphoImager technology. Activity measurements are performed in duplicates or triplicates with less than 10% difference between replicates. Experiments are repeated at least twice[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    Human renal mesangial cells (HRMCs) are cultured with 1640 media, containing 10% fetal bovin serum at 37 °C in 5% CO2. Cells are cultured with D-glucose at normal (5.5 mM) or high (25 mM) concentrations in serum-free medium. D-Mannitol (25 mM) is used for a control of osmolality. TP is reconstituted in 0.01% DMSO and freshly diluted with culture medium to 10 ug/L before using. To determine the specific role of PDK1 in TP-potentiated anti-proliferation, 5 μM PS48 (MedChem Express, USA) is applied following the treatment of TP. MTT assay is used to detect cell proliferation. HRMCs are seeded at a density of 1x105/mL into 96-well plates. After 12, 24, 48 and 72 h incubation with different compounds, 20 uL MTT (5 mg/mL) is added to each well. Cells are then cultured for an additional 2 h and subsequently lysed using DMSO (150 uL/well). When the formazan crystals completely dissolve, the optical density (OD) is measured at 570 nm. The arithmetic mean OD of six wells for each group is calculated[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    PS48 相关分类

    完整储备液配制表

    * 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。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.4874 mL 17.4368 mL 34.8736 mL 87.1840 mL
    5 mM 0.6975 mL 3.4874 mL 6.9747 mL 17.4368 mL
    10 mM 0.3487 mL 1.7437 mL 3.4874 mL 8.7184 mL
    15 mM 0.2325 mL 1.1625 mL 2.3249 mL 5.8123 mL
    20 mM 0.1744 mL 0.8718 mL 1.7437 mL 4.3592 mL
    25 mM 0.1395 mL 0.6975 mL 1.3949 mL 3.4874 mL
    30 mM 0.1162 mL 0.5812 mL 1.1625 mL 2.9061 mL
    40 mM 0.0872 mL 0.4359 mL 0.8718 mL 2.1796 mL
    50 mM 0.0697 mL 0.3487 mL 0.6975 mL 1.7437 mL
    60 mM 0.0581 mL 0.2906 mL 0.5812 mL 1.4531 mL
    80 mM 0.0436 mL 0.2180 mL 0.4359 mL 1.0898 mL
    100 mM 0.0349 mL 0.1744 mL 0.3487 mL 0.8718 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PS481180676-32-7PS 48PS-48PDK-13-Phosphoinositide-dependent protein kinase 1Inhibitorinhibitorinhibit

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