2. JAK/STAT Signaling Stem Cell/Wnt
  3. STAT
  4. NSC 74859

NSC 74859  (Synonyms: S3I-201)

目录号: HY-15146 纯度: 98.64%
COA 产品使用指南

摩尔计算器

NSC 74859 (S3I-201) 是选择性的 Stat3 抑制剂，IC50 为 86 μM。

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NSC 74859 Chemical Structure

NSC 74859 Chemical Structure

CAS No. : 501919-59-1

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规格 价格 是否有货 数量
1 mg ￥250
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5 mg ￥500
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10 mg ￥700
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50 mg ￥1750
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100 mg ￥3300
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500 mg   询价  

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Customer Review

NSC 74859 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 46 篇科研文献

WB

    NSC 74859 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2023 Feb 27;42(1):51.  [Abstract]

    The enhanced phosphorylation level of JAK2 and STAT3 mediated by rhCCL18 can be reversed by NSC 74859 (S3I-201) in EC-109, EC-109 Vector and EC-109 shPITPNM3 cells.

    NSC 74859 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 28;430:201-214.  [Abstract]

    CD146WT or CD146KO MEFs are stimulated with or without TGF-β1 (10 ng/mL) for 24 h in the presence or absence of NSC74859 (200 μM). The expression of CD146, the expression and activation of STAT3, and the expression levels of E-cadherin, N-cadherin, and Twist are assessed by immunoblotting.

    NSC 74859 purchased from MCE. Usage Cited in: Biofactors. 2018 Nov;44(6):570-576.  [Abstract]

    Westen Blot analysis of HMGB1 expression in HepG2 cells in the treatment of Stat3 inhibitor NSC74859 (SI3), or activator (NAC).

    NSC 74859 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Aug 30.  [Abstract]

    AA-FLS are treated with different concentrations (25, 50, and 100 µM) of Ferulic acid (FA) and 50 µM of S3I-201 and then cultured in the presence or absence of IL-17 (10 ng/mL). The cell lysates are subjected to Western blot analysis to assess the expression levels of TLR-3, Cyr61, IL-23 and GM-CSF proteins.

    NSC 74859 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Nov;91:134-144.  [Abstract]

    AA-FLS cultured in the presence or absence of S3I-201 for 24 h, then treated with IL-17 for an additional 24 h and phosphorylation of STAT-3 is detected by western blotting.

    查看 STAT 亚型特异性产品:

    查看所有亚型
    STAT3 STAT5 STAT6 STAT1

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM[1].

    IC50 & Target[1]

    STAT3

    86 μM (IC50)

    体外研究
    (In Vitro)

    NSC 74859 (S3I-201) preferentially inhibits Stat3 DNA-binding activity over that of Stat1 (IC50 values, Stat3•Stat3, 86±33 μM; Stat1•Stat3, 160±43 μM; and Stat1•Stat1, >300 μM) and inhibits that of Stat5 with IC50 of 166±17 μM). NSC 74859 significantly reduces viable cell numbers and inhibits growth of transformed mouse fibroblasts NIH 3T3/v-Src and breast carcinoma cell lines (MDA-MB-231, MDA-MB-435, and MDA-MB-468). At 30-100 μM, NSC 74859 induces significant apoptosis in the representative human breast carcinoma cell line MDA-MB-435 and NIH 3T3/v-Src, both of which harbor constitutively active Stat3. The breast carcinoma MDA-MB-435 cell line is more sensitive to 30 μM NSC 74859. By contrast, the human breast cancer MDA-MB-453 cells and the normal mouse fibroblasts (NIH 3T3), which do not contain abnormal Stat3 activity, are less sensitive to NSC 74859 at 100 μM or less. At 300 μM or higher, NSC 74859 induced general, nonspecific cytotoxicity independent of Stat3 activation status[1]. Huh-7 cells do not express β2SP or TBGFR2 and are sensitive to STAT3 inhibition, with an IC50 of 100 μM for NSC 74859, regardless of CD133+ status. The IC50 of NSC 74859 is 150 μM for Huh-7 and SNU-398 cells, 15 μM for SNU-475 cells and 200 μM for SNU-182 cells. NSC 74859 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with an IC50 close to 100 μM[2].

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

    NSC 74859 相关抗体:
    体内研究
    (In Vivo)

    Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, and tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth[1]. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm3 vs. 287±16 mm3, P<0.01) as early as 5 days after NSC 74859 injection. Fifteen days after treatments, the average tumor volume of NSC 74859-treated rats is 64% of that of controls (449±40 mm3 vs. 708±83 mm3, P<0.01). Rats are sacrificed and tumors are harvested 15 days after treatment initiation. The average tumor weight of NSC 74859-treated rats is 78±8 mg, while tumors derived from control rats weighed 114±13 mg (32% reduction; P<0.05)[3].

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

    365.36

    Formula

    C16H15NO7S
    CAS 号
    性状

    固体

    颜色

    White to gray

    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

    *该产品在溶液状态不稳定，建议您现用现配，即刻使用。

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (273.70 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 2.7370 mL 13.6851 mL 27.3703 mL
    5 mM 0.5474 mL 2.7370 mL 5.4741 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

    • 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: ≥ 7.5 mg/mL (20.53 mM); 澄清溶液

      此方案可获得 ≥ 7.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 7.5 mg/mL (20.53 mM); 澄清溶液

      此方案可获得 ≥ 7.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 75.0 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）。

    *该产品在溶液状态不稳定，建议您现用现配，即刻使用。

    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: 98.64%

    COA (195 KB) LCMS (269 KB)

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

    Proliferating cells are treated with or without NSC 74859 (30-100 μM) for up to 48 h. In some cases, cells are first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24-48 h. Cells are then detached and analyzed by annexin V binding and flow cytometry to quantify the percent apoptosis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    Six-week-old female athymic nude mice are used. Athymic nude mice are injected in the left flank area s.c. with 5×106 human breast cancer MDA-MB-231 cells in 100 μL of PBS. After 5-10 days, tumors with a diameter of 3 mm are established. Animals are given NSC 74859 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals are stratified so that the mean tumor sizes in all treatment are nearly identical. Tumor volume is calculated according to the formula V=0.52×a2×b, where a is the smallest superficial diameter and b is the largest superficial diameter.
    Rats[3]
    Four-week-old female Wistar Furth rats are used. GH3 cells (5×105 cells in 100 μL Matrigel) are subcutaneously injected into the left lumbar area. After 7 days, tumors with a volume of approximately 100 mm3 are established. Rats are given NSC 74859 intravenously at 5 mg/kg every 2 or 3 days for 2 weeks. Tumor size is measured by caliper measurements twice a week, and volume is calculated as follows: volume=(length×width2)/2. Three weeks after cell inoculations, animals are euthanized and excised tumors are weighed. Blood samples are collected 1 day before S3I-201 treatment and again on the day of euthanization. Serum GH and prolactin are assessed by RIA or ELISA, respectively.

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

    NSC 74859 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7370 mL 13.6851 mL 27.3703 mL 68.4257 mL
    5 mM 0.5474 mL 2.7370 mL 5.4741 mL 13.6851 mL
    10 mM 0.2737 mL 1.3685 mL 2.7370 mL 6.8426 mL
    15 mM 0.1825 mL 0.9123 mL 1.8247 mL 4.5617 mL
    20 mM 0.1369 mL 0.6843 mL 1.3685 mL 3.4213 mL
    25 mM 0.1095 mL 0.5474 mL 1.0948 mL 2.7370 mL
    30 mM 0.0912 mL 0.4562 mL 0.9123 mL 2.2809 mL
    40 mM 0.0684 mL 0.3421 mL 0.6843 mL 1.7106 mL
    50 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3685 mL
    60 mM 0.0456 mL 0.2281 mL 0.4562 mL 1.1404 mL
    80 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
    100 mM 0.0274 mL 0.1369 mL 0.2737 mL 0.6843 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:

    NSC 74859501919-59-1S3I-201NSC74859NSC-74859STATInhibitorinhibitorinhibit

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