1. Immunology/Inflammation
  2. SOD
  3. ATN-224

ATN-224  (Synonyms: Bis(choline)tetrathiomolybdate)

目录号: HY-16074 纯度: ≥98.0%
COA 产品使用指南

ATN-224 是一种Cu2+/Zn2+-超氧化物歧化酶 1 (SOD1) 抑制剂。ATN-224 作用内皮细胞,抑制抑制SOD1活性,IC50 为 17.5±3.7 nM。

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ATN-224 Chemical Structure

ATN-224 Chemical Structure

CAS No. : 649749-10-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3098
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2 mg ¥1600
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5 mg ¥3255
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10 mg ¥4650
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Top Publications Citing Use of Products

    ATN-224 purchased from MCE. Usage Cited in: Anal Chem. 2018 Jan 16;90(2):1317-1324.  [Abstract]

    Illumination of the ・OH release along the deactivation of SOD1 by enzyme inhibitor ATN-224. The RAW 264.7 cells are treated by 100 μM ATN-224 for 0, 2, 6, 18 h, and then incubated with 10 μM P2 for 30 min. Scale bar: 10 μm. Fluorescence intensity (F) is displayed as yellow bars.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM.

    IC50 & Target

    IC50: 17.5±3.7 nM (SOD1, in endothelial cells)[1]

    体外研究
    (In Vitro)

    ATN-224 has a specific and high affinity for copper ions (108 mol/L-1) and shows no binding to calcium, iron, magnesium, zinc, or manganese ions at concentrations up to 1 mM as determined by isothermal titration calorimetry. ATN-224 inhibits the proliferation of both HUVEC (IC50=1.4±0.3 μM; n=5). ATN-224 is also able to inhibit the activity of purified bovine SOD1 with an IC50 of 0.33±0.03 μM after 24 hours of incubation. The SOD1 inhibition by ATN-224 is time dependent, reaching maximal inhibition at ~16 hours. ATN-224 seems to inhibit SOD1 by depleting the enzyme of copper. ATN-224 is able to inhibit SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 inhibits FGF-2-induced ERK1/2 phosphorylation in a dose-dependent and time-dependent manner with an IC50 between 1.25 and 2.5 μM, consistent with the IC50 for the inhibition of proliferation[1]. ATN-224 is an orally-available inorganic small molecule that inhibits the copper/zinc-dependent enzyme, superoxide dismutase 1 (Cu/Zn-SOD1), in endothelial and tumor cells[2].

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

    体内研究
    (In Vivo)

    ATN-224 also significantly (P<0.05) inhibits angiogenesis in the Matrigel plug model in mice either when added directly to the plug or when given by oral gavage. Inhibition of angiogenesis when ATN-224 is given by oral gavage occurred before there is measurable depletion of copper in either plasma or copper from the Matrigel plug. This result shows that ATN-224 inhibits angiogenesis independently of copper depletion[1].

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

    分子量

    432.56

    Formula

    C10H28MoN2O2S4

    CAS 号
    性状

    固体

    颜色

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

    DMSO 中的溶解度 : 50 mg/mL (115.59 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 2.3118 mL 11.5591 mL 23.1182 mL
    5 mM 0.4624 mL 2.3118 mL 4.6236 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 (5.78 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。

      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 (5.78 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。

      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

    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: ≥98.0%

    参考文献
    Kinase Assay
    [1]

    Cells are plated in a six-well format (100-300,000 per well) and incubated with ATN-224 at indicated concentrations and for indicated times. Cells are then stimulated with 10 ng/mL FGF-2 for various times and lysed. Lysates are subjected to Western blot analysis using an antibody specific for phosphorylated p44/42 mitogen-activated protein kinase (Thr202/Tyr204) with appropriate signal correction using an antibody specific for p44/42 mitogen-activated protein kinase[1].

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

    Cell Assay
    [1]

    Human umbilical vein endothelial cells (HUVEC) are maintained in M200/LSGS medium and cells are used between passages 2 and 4 for all experiments. For proliferation assay, cells are plated at 3,000 per well on 0.1% gelatin in M200/2% FBS for 4 hours and then stimulated with 2 ng/mL FGF-2 in the presence or absence of ATN-224 up to 48 hours. HUVEC proliferation is determined using either the Alamar Blue or the MTT assay. Multiple myeloma MM1S cells are grown in RPMI 1640 with 10% fetal bovine serum and 2 mM L-glutamine. HL-60 promyelocytic leukemia cells and MOLT-4 acute myeloblastic leukemia cells are plated at 400,000/mL in T-75 flasks and incubated for 48 to 96 hours for proliferation assays. MMS1 cell proliferation is determined using calcein AM[1].

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

    Animal Administration
    [1]

    Mice[1]
    Cold Matrigel (500 μL) is mixed with 800 ng/mL FGF-2 or 300 ng/mL VEGF and heparin (50 μg/mL). Negative control plugs did not contain the proangiogenic factors. The Matrigel mixture is injected s.c. into 4- to 8-week-old female BALB/c nude mice. In some experiments, either ATN-224 (94 μM) with or without Mn-TBAP (100 μM) or water is added directly to the Matrigel plug in the treated and negative control groups, respectively. Alternatively, mice are treated by oral gavage either with distilled water or ATN-224 everyday from Monday to Friday. Animals are sacrificed and the plugs are recovered 5 days after plug injection. The plugs are then minced and homogenized with a tissue homogenizer, and hemoglobin levels in the plugs are determined using Drabkin's solution.

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

    参考文献

    ATN-224 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 2.3118 mL 11.5591 mL 23.1182 mL 57.7955 mL
    5 mM 0.4624 mL 2.3118 mL 4.6236 mL 11.5591 mL
    10 mM 0.2312 mL 1.1559 mL 2.3118 mL 5.7795 mL
    15 mM 0.1541 mL 0.7706 mL 1.5412 mL 3.8530 mL
    20 mM 0.1156 mL 0.5780 mL 1.1559 mL 2.8898 mL
    25 mM 0.0925 mL 0.4624 mL 0.9247 mL 2.3118 mL
    30 mM 0.0771 mL 0.3853 mL 0.7706 mL 1.9265 mL
    40 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4449 mL
    50 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1559 mL
    60 mM 0.0385 mL 0.1927 mL 0.3853 mL 0.9633 mL
    80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7224 mL
    100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
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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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    产品名称:
    ATN-224
    目录号:
    HY-16074
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