2. Apoptosis
  3. PKD
  4. CID755673

CID755673 是高效选择性的 PKD1 抑制剂，IC50 值为 182 nM。

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CID755673 Chemical Structure

CID755673 Chemical Structure

CAS No. : 521937-07-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
1 mg ￥272
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5 mg ￥600
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10 mg ￥900
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50 mg ￥2500
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100 mg ￥4500
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500 mg   询价  

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Customer Review

CID755673 相关抗体

Top Publications Citing Use of Products

    CID755673 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287.  [Abstract]

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.

    CID755673 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.

    Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with Western blot analysis.

    CID755673 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.

    Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with RT-PCR.

    CID755673 purchased from MCE. Usage Cited in: Chinese Journal of Pathophysiology. 2016, 32(1):146-150, 155.

    The effects of PKD1 on the mRNA and protein expression of VEGF and KDR in the endothelial progenitor cells ( EPCs).

    查看 PKD 亚型特异性产品:

    查看所有亚型
    PKD1 PKD2 PKD3

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

    IC50 & Target[1]

    PKD1

    182 nM (IC50)

    PKD3

    227 nM (IC50)

    PKD2

    280 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    LNCaP IC50
    11.8 μM
    Compound: CID755673
    Inhibition of PKD1 autophosphorylation at Ser916 in human PMA-induced LNCAP cells by Western blotting
    Inhibition of PKD1 autophosphorylation at Ser916 in human PMA-induced LNCAP cells by Western blotting
    		[PMID: 21617763]
    体外研究
    (In Vitro)

    CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation, cell migration, and invasion[1].

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

    CID755673 相关抗体:
    体内研究
    (In Vivo)

    Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 administration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight[2].

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

    217.22

    Formula

    C12H11NO3
    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (460.36 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.6036 mL 23.0181 mL 46.0363 mL
    5 mM 0.9207 mL 4.6036 mL 9.2073 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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 (11.51 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 (11.51 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

    纯度: 99.13%

    COA (290 KB) LCMS (96 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μL of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range[1].

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

    The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cells are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a ×10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a final image[1].

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

    Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/kg body weight. Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection[2].

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

    CID755673 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.6036 mL 23.0181 mL 46.0363 mL 115.0907 mL
    5 mM 0.9207 mL 4.6036 mL 9.2073 mL 23.0181 mL
    10 mM 0.4604 mL 2.3018 mL 4.6036 mL 11.5091 mL
    15 mM 0.3069 mL 1.5345 mL 3.0691 mL 7.6727 mL
    20 mM 0.2302 mL 1.1509 mL 2.3018 mL 5.7545 mL
    25 mM 0.1841 mL 0.9207 mL 1.8415 mL 4.6036 mL
    30 mM 0.1535 mL 0.7673 mL 1.5345 mL 3.8364 mL
    40 mM 0.1151 mL 0.5755 mL 1.1509 mL 2.8773 mL
    50 mM 0.0921 mL 0.4604 mL 0.9207 mL 2.3018 mL
    60 mM 0.0767 mL 0.3836 mL 0.7673 mL 1.9182 mL
    80 mM 0.0575 mL 0.2877 mL 0.5755 mL 1.4386 mL
    100 mM 0.0460 mL 0.2302 mL 0.4604 mL 1.1509 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:

    CID755673521937-07-5CID 755673CID-755673PKDProtein kinase DInhibitorinhibitorinhibit

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    目录号：
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