1. Stem Cell/Wnt TGF-beta/Smad
  2. TGF-beta/Smad
  3. SIS3

SIS3  (Synonyms: SIS3 盐酸盐)

目录号: HY-13013 纯度: 98.71%
COA 产品使用指南

(E)-SIS3 是一种有效和选择性的 Smad3 抑制剂,抑制 Smad3 磷酸化的 IC50 为 3 μM。(E)-SIS3 通过 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。

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SIS3 Chemical Structure

SIS3 Chemical Structure

CAS No. : 521984-48-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1186
In-stock
2 mg ¥750
In-stock
5 mg ¥1100
In-stock
10 mg ¥1900
In-stock
25 mg ¥3500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 71 篇科研文献

WB

    SIS3 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Aug;20(2):1605-1612.  [Abstract]

    SIS3 treatment decreases the TGFβ1-induced expression of Col I and FN.

    SIS3 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.  [Abstract]

    NRK-49F cells are preincubated with 100 nM, 10 μM, or 50 μM Smad3 inhibitor SIS3 for 30 min followed by TGF-β1 (2 ng/mL) stimulation for 12 h. Then, the expression of Sphk2, fibronectin, and α-SMA is determined by Western blotting.

    SIS3 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    SIS3 purchased from MCE. Usage Cited in: Int J Mol Med. 2019 Feb;43(2):993-1002.   [Abstract]

    Western analysis of FN expression in HUVECs pretreated with PD98059 and SIS3.

    SIS3 purchased from MCE. Usage Cited in: Immunol Lett. 2019 Feb;206:33-40.  [Abstract]

    Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.

    SIS3 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov;103:173-181.  [Abstract]

    TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.

    SIS3 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.

    CNE1 cells are cultured with 3 μM SIS3 for 4 hs, and then washed by cold PBS and followed by the 10 ng/mL TGF-β treatments for 48 hs, respectively.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1[1].

    IC50 & Target

    IC50: 3 μM (Smad3 phosphorylation)[1]

    体外研究
    (In Vitro)

    (E)-SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1].
    (E)-SIS3 (0.1 , 10, 50 μM; 30 min) significantly suppresses the expression of FN and α-SMA, but not that of Sphk2 provoked by TGF-β1[2].
    (E)-SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts[3].
    (E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 µM to 50 µM (5 µM, 10 µM, 20 µM and 50 µM) in a dose-dependent manner[4].

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

    Western Blot Analysis[1]

    Cell Line: Human dermal fibroblasts
    Concentration: 0.3, 1, 3, 10 μM
    Incubation Time: For 1 hour
    Result: Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
    分子量

    489.99

    Formula

    C28H28ClN3O3

    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    SIS3 盐酸盐

    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, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (255.11 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 2.0409 mL 10.2043 mL 20.4086 mL
    5 mM 0.4082 mL 2.0409 mL 4.0817 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 (sealed storage, away from moisture)。-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

    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: ≥ 2.08 mg/mL (4.24 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。
    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)。

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    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: 98.71%

    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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-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 2.0409 mL 10.2043 mL 20.4086 mL 51.0215 mL
    5 mM 0.4082 mL 2.0409 mL 4.0817 mL 10.2043 mL
    10 mM 0.2041 mL 1.0204 mL 2.0409 mL 5.1021 mL
    15 mM 0.1361 mL 0.6803 mL 1.3606 mL 3.4014 mL
    20 mM 0.1020 mL 0.5102 mL 1.0204 mL 2.5511 mL
    25 mM 0.0816 mL 0.4082 mL 0.8163 mL 2.0409 mL
    30 mM 0.0680 mL 0.3401 mL 0.6803 mL 1.7007 mL
    40 mM 0.0510 mL 0.2551 mL 0.5102 mL 1.2755 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0204 mL
    60 mM 0.0340 mL 0.1701 mL 0.3401 mL 0.8504 mL
    80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6378 mL
    100 mM 0.0204 mL 0.1020 mL 0.2041 mL 0.5102 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.

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    产品名称:
    SIS3
    目录号:
    HY-13013
    需求量: