2. PI3K/Akt/mTOR Stem Cell/Wnt Autophagy
  3. GSK-3 Autophagy
  4. SB 216763

SB 216763是有效，选择性和ATP竞争性的 GSK-3 抑制剂，抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。

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SB 216763 Chemical Structure

SB 216763 Chemical Structure

CAS No. : 280744-09-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥715
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1 mg ￥295
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5 mg ￥650
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10 mg ￥1100
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50 mg ￥4800
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100 mg ￥7886
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Customer Review

SB 216763 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 29 篇科研文献

WB
IF

    SB 216763 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Apr;150:280-292.  [Abstract]

    Expression of c-Myc in MKN-45 cells treated with Lanatoside C and SB216763 at indicated concentrations for 24 h.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Representative micrographs showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Cardiac protein expression of LC3-I, LC3-II, and p62 are assayed in cardiac tissues treated with Aldo-salt or with Aldo-salt plus SB-216763.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Renal protein expression of LC3-I, LC3-II and p62 are assayed in renal tissues treated with Aldo-salt or with Aldo-salt plus SB-216763. SB-216763 increased the Aldo-salt-induced autophagy.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Images showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MCE. Usage Cited in: Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.  [Abstract]

    SB 216763 blocks augmentation of phosphor-glycogen synthase and depletion of inhibitory phosphorylated GSK-3β at serine 9 sites, but maintains total GSK-3β levels. Cardiac protection following SB 216763 is dependent on GSK-3β activity inhibition, not on decrease in basal GSK-3β levels. H9c2 cells are treated with 160 nM TP for 24 h after pretreatments with 2 μM SB 216763 or vehicle 2 h later. Levels of p-GS, p-GSK-3β, GSK-3β and GAPDH are measured by western blot.

    查看 GSK-3 亚型特异性产品:

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    GSK-3 GSK-3α GSK-3β

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

    IC50 & Target[5]

    GSK-3α

    34.3 nM (IC50)

    GSK-3β

    34.3 nM (IC50)

    体外研究
    (In Vitro)

    SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month[2].
    SB-216763 inhibits GSK-3 with IC50 of 34 nM[3].
    SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].

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

    SB 216763 相关抗体:
    体内研究
    (In Vivo)

    SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO[4].

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

    371.22

    Formula

    C19H12Cl2N2O2
    CAS 号
    性状

    固体

    颜色

    Orange to red

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (269.38 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 2.6938 mL 13.4691 mL 26.9382 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 (6.73 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 (6.73 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      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

    纯度: 99.82%

    COA (203 KB) HNMR (289 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    MESCs maintained with LIF or 10 µM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 µL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2 inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).

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

    SB 216763 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 2.6938 mL 13.4691 mL 26.9382 mL 67.3455 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 mL 13.4691 mL
    10 mM 0.2694 mL 1.3469 mL 2.6938 mL 6.7346 mL
    15 mM 0.1796 mL 0.8979 mL 1.7959 mL 4.4897 mL
    20 mM 0.1347 mL 0.6735 mL 1.3469 mL 3.3673 mL
    25 mM 0.1078 mL 0.5388 mL 1.0775 mL 2.6938 mL
    30 mM 0.0898 mL 0.4490 mL 0.8979 mL 2.2449 mL
    40 mM 0.0673 mL 0.3367 mL 0.6735 mL 1.6836 mL
    50 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3469 mL
    60 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1224 mL
    80 mM 0.0337 mL 0.1684 mL 0.3367 mL 0.8418 mL
    100 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 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:

    SB 216763280744-09-4SB216763SB-216763GSK-3AutophagyGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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