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  2. PDHK Reactive Oxygen Species NKCC Apoptosis
  3. Sodium dichloroacetate

Sodium dichloroacetate  (Synonyms: 二氯乙酸钠)

目录号: HY-Y0445A 纯度: 99.76%
COA 产品使用指南 技术支持

Sodium dichloroacetate 是癌细胞线粒体中的一种代谢调节剂,具有抗癌活性。Sodium dichloroacetate 抑制丙酮酸脱氢酶激酶 (PDHK),从而导致肿瘤微环境中的乳酸减少。Sodium dichloroacetate 增加活性氧 (ROS) 的产生并促进癌细胞凋亡,还可作为 NKCC 抑制剂。

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Sodium dichloroacetate Chemical Structure

Sodium dichloroacetate Chemical Structure

CAS No. : 2156-56-1

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Customer Review

Other Forms of Sodium dichloroacetate:

    Sodium dichloroacetate purchased from MCE. Usage Cited in: Life Sciences. 2022: 121192.

    Sodium dichloroacetate (DCA; 10 mM; 48 h) significantly inhibits hypoxia-induced proliferation of HPASMCs (Fig I) , and markedly increases the apoptosis rate (Fig J).
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor[1].

    IC50 & Target

    PDHK; Reactive oxygen species (ROS); Apoptosis; NKCC[1]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    4T1 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against mouse 4T1 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against mouse 4T1 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    A-375 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human A375 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human A375 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    A-375 IC50
    20.1 mM
    Compound: DCA
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    A549 IC50
    1011 μM
    Compound: DCA
    Anticancer activity against human A549 cells after 72 hrs by MTT assay
    Anticancer activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    A549 IC50
    19.5 mM
    Compound: DCA
    Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    A549 IC50
    20.1 mM
    Compound: DCA
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30470491]
    A549 IC50
    23.58 mM
    Compound: DCA
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27006991]
    A549 IC50
    4286 μM
    Compound: DCA
    Cytotoxicity against human A549 cells after 68 hrs by MTT assay
    Cytotoxicity against human A549 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    Bel-7402 IC50
    860 μM
    Compound: DCA
    Anticancer activity against human Bel7402 cells after 72 hrs by MTT assay
    Anticancer activity against human Bel7402 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    BGC-823 IC50
    1051 μM
    Compound: DCA
    Anticancer activity against human BGC823 cells after 72 hrs by MTT assay
    Anticancer activity against human BGC823 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    HCT-116 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human HCT116 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human HCT116 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    HCT-116 IC50
    9.8 mM
    Compound: DCA
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    KB IC50
    1424 μM
    Compound: DCA
    Anticancer activity against human KB cells after 72 hrs by MTT assay
    Anticancer activity against human KB cells after 72 hrs by MTT assay
    [PMID: 20663593]
    KB 3-1 IC50
    5883 μM
    Compound: DCA
    Cytotoxicity against human KB-3-1 cells after 68 hrs by MTT assay
    Cytotoxicity against human KB-3-1 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    L02 IC50
    > 100 μM
    Compound: Na-DCA
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    L02 IC50
    21.7 mM
    Compound: DCA
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33550182]
    MCF7 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human MCF7 cells overexpressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human MCF7 cells overexpressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    MCF7 IC50
    12.35 mM
    Compound: DCA
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27006991]
    MCF7 IC50
    13.4 mM
    Compound: DCA
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    NCI-H1650 IC50
    16.3 mM
    Compound: DCA
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30470491]
    NCI-H460 IC50
    3892 μM
    Compound: DCA
    Cytotoxicity against human H460 cells after 68 hrs by MTT assay
    Cytotoxicity against human H460 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    PC-3 IC50
    15.7 mM
    Compound: DCA
    Antiproliferative activity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    SH-SY5Y IC50
    17.4 mM
    Compound: DCA
    Antiproliferative activity against human SHSY-5Y cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human SHSY-5Y cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    体外研究
    (In Vitro)

    Sodium dichloroacetate 可增加线粒体中的 ROS 生成。Sodium dichloroacetate 通过促进氧化代谢而增加 ROS 生成,从而影响细胞生长和活力。Sodium dichloroacetate 对多发性骨髓瘤细胞活力、细胞周期停滞和细胞凋亡的影响与丙酮酸脱氢酶激酶 (PDK) 抑制、丙酮酸脱氢酶 (PDH) 活性恢复以及促进氧化代谢有关,同时还与细胞内 ROS 生成增加有关,而细胞内 ROS 生成增加取决于 Sodium dichloroacetate 的剂量。Sodium dichloroacetate 作用与 CI 抑制协同促进大鼠 VM-M3 胶质母细胞瘤细胞中的氧化应激。经 Sodium dichloroacetate 处理的癌细胞中 ROS 水平升高与诱导凋亡有关,而凋亡与细胞色素 c 表达增加有关。Sodium dichloroacetate 导致 ROS 依赖性 T 细胞分化[1]

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

    体内研究
    (In Vivo)

    Sodium dichloroacetate 处理的性腺完整和阉割的雄性大鼠中 NKCC1 RNA 表达水平显著降低,而 Sodium dichloroacetate 处理的性腺完整和阉割的雌性大鼠中没有发现这种影响[1]
    单剂量 Sodium dichloroacetate 可显著增加 Wistar 雄性大鼠的 24 小时利尿量,而利尿量的增加与 NKCC2 抑制有关。与完整雄性大鼠相比,完整雌性大鼠肾脏中的 NKCC2 更丰富,Sprague-Dawley 雌性大鼠的转运蛋白密度更高[1]
    口服 5、20 和 100 mg/kg Sodium dichloroacetate 在雄性大鼠体内的生物利用度显著低于 GSTζ 缺乏的大鼠(分别为 10%、13%、81% 和 31%、75%、100%)。GSTζ 缺乏的大鼠体内 Sodium dichloroacetate 的肝脏提取具有线性动力学,但在较高剂量下随着代谢饱和而降低[1]

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

    Clinical Trial
    分子量

    150.92

    Formula

    C2HCl2NaO2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    二氯乙酸钠

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    H2O 中的溶解度 : 100 mg/mL (662.60 mM; 超声助溶)

    DMSO 中的溶解度 : 25 mg/mL (165.65 mM; 超声助溶 (<60°C); 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 6.6260 mL 33.1301 mL 66.2603 mL
    5 mM 1.3252 mL 6.6260 mL 13.2521 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 (sealed storage, away from moisture)。-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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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:

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

      Solubility: 100 mg/mL (662.60 mM); 澄清溶液; 超声助溶

    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

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.76%

    参考文献

    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 (sealed storage, away from moisture)。-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 / H2O 1 mM 6.6260 mL 33.1301 mL 66.2603 mL 165.6507 mL
    5 mM 1.3252 mL 6.6260 mL 13.2521 mL 33.1301 mL
    10 mM 0.6626 mL 3.3130 mL 6.6260 mL 16.5651 mL
    15 mM 0.4417 mL 2.2087 mL 4.4174 mL 11.0434 mL
    20 mM 0.3313 mL 1.6565 mL 3.3130 mL 8.2825 mL
    25 mM 0.2650 mL 1.3252 mL 2.6504 mL 6.6260 mL
    30 mM 0.2209 mL 1.1043 mL 2.2087 mL 5.5217 mL
    40 mM 0.1657 mL 0.8283 mL 1.6565 mL 4.1413 mL
    50 mM 0.1325 mL 0.6626 mL 1.3252 mL 3.3130 mL
    60 mM 0.1104 mL 0.5522 mL 1.1043 mL 2.7608 mL
    80 mM 0.0828 mL 0.4141 mL 0.8283 mL 2.0706 mL
    100 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6565 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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    • 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.

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