SIS3 HCl

For research use only. Not for use in humans.

目录号:S7959

SIS3 HCl Chemical Structure

CAS No. 521984-48-5

SIS3是一种新型的特异性Smad3抑制剂,通过抑制Smad3的磷酸化抑制TGF-β和activin信号,而不影响MAPK/p38, ERK或PI3-kinase信号通路。

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客户使用Selleck生产的SIS3 HCl发表文献35篇:

产品安全说明书

TGF-beta/Smad抑制剂选择性比较

生物活性

产品描述 SIS3是一种新型的特异性Smad3抑制剂,通过抑制Smad3的磷酸化抑制TGF-β和activin信号,而不影响MAPK/p38, ERK或PI3-kinase信号通路。
靶点
Smad3 [1]
()
体外研究

SIS3通过降低转录活性、减弱TGF-β1的效果。SIS3抑制成纤维细胞的肌成纤维细胞分化,在硬皮病成纤维细胞中,减少Smad3组成型磷酸化以及上调的I型胶原,从而在体外TGF-β1相关的正常皮肤成纤维细胞和硬皮病成纤维细胞中阻止ECM的过表达[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HK-2 cell MYDD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MUK15qCK|ryP MkXLNUBp M{DhUXRz\WG2bXXueEB4cXSqIGPJV|Mhe3WycILld5Nm\CClYXTtbZVuNWmwZIXj[YQhUEtvMjDj[YxtKGSnYYToMi=> NYP1bm92OzB6MES0O|A>
A549 cells MWnGeY5kfGmxbjDhd5NigQ>? MnvuN{DPxE1? NHLERZVVcGViY3XscJMhcW5idHjlJHNKWzNiZ4LveZAh\Gm|cHzhfYVlKGFic4DpcoRt\S2|aHHw[YQh\WyxbnfheIVlKG[rYoLvZoxie3RvbHnr[UBud3KyaH;sc4d6Ng>? NHTTSZYzQTJyN{C1OS=>
AML12 cell line M3\ZOGZ2dmO2aX;uJIF{e2G7 M4LxclExKM7:TR?= MmPhN|AhdWmwcx?= MkjaV2lUOyCkbH;jb5MhXEeILd8yMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBUVUGGMzDhcoQhfGinIITveIFtKFOPQVSyM|MhdGW4ZXzzJIFz\SC3bnPoZY5o\WRw MlvKNlc1PjJyN{W=
A549 cells NFrXU3lHfW6ldHnvckBie3OjeR?= MoXyN{DPxE1? M4nyZ|QhcA>? MWnTTXM{KHOrZ37p[olk[W62bImgdoV{fG:{ZXSgSU1k[WSqZYLpckBmgHC{ZYPzbY9vKGGwZDDpcZBicXKnZDD2bY1mdnSrbjDhcoQhW26jaXyg[ZhxemW|c3nvckBqdiC2aHWgdJJme2WwY3Wgc4YhXEeILd8yNU4> M4DPUVI1PTd|MEO4
MCF-7 cells NIPIdVRRem:uaX\ldoF1cW:wIHHzd4F6 NHGxOogzNjVizszN MXnjc45kfXK{ZX70JJRz\WG2bXXueEB4cXSqIGPJV|MhemWmdXPl[EB1cGViaX7obYJqfG:{eTDl[oZm[3Rib3[g[Yxt[WerYzDhZ4llKG:wIITo[UBxem:uaX\ldoF1cW:wIH;mJG1ETi15IHLy[YF{fCClYX7j[ZIh[2WubIOu M1fxRlI1PTJ6MEO4

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
COX-2 / HMGB1; 

PubMed: 24098479     


SB431542 (10 µM) or SIS3 (30 µM) blocked TGF-β1-induced COX-2 downregulation. Cells were pretreated for 60 min with the inhibitor, and then incubated with or without TGF-β1 (5 ng/mL) for 24 h. 

p-Smad3 / Smad3 / E-cadherin / Ck18 / Fibronectin / MMP9; 

PubMed: 23430956     


Representative western blots of E-cadherin, CK18, fibronectin and MMP-9 in HepG2 and BEL7402 cells with or without SIS3.

24098479 23430956
Immunofluorescence
KDEL / Fibronectin; 

PubMed: 29743238     


Inhibition of TGFβ signaling blocks Dex-induced intracellular fibronectin co-localization with ER stress markers in primary human TM cells. Primary human TM cells (n = 3 cell strains) were treated with Veh or Dex in the presence or absence of TGFβ-signaling inhibitors (LY364947 and SIS3) for 72 h, and cells were stained for fibronectin and KDEL (Triton-permeabilized cells). The Dex-induced intracellular fibronectin load and its co-localization with KDEL were completely blocked by TGFβ-signaling inhibitors. Scale bar = 50 micron.

α-SMA / Vimentin; 

PubMed: 25793924     


Effect of LY364947 and SIS3 on the expression of EMT markers altered by TGFβ1, seen by Immunofluorescence.

p-Smad3; 

PubMed: 29207055     


Localization of p-Smad3 occurs in the cells as shown by immunofluorescence. p-Smad3 is shown in red, TRITC-stained; counterstaining of nuclei with DAPI is shown in blue. Scale bar, 50 μm. The cell groups were as follows: control, cells cultured in serum-free DMEM; TGF-β1, cells cultured in serum-free DMEM and exposed to 5 ng/ml TGF-β1; SIS3, cells were treated with 3 μM SIS3 (specific inhibitor of Smad3) which was added 4 h prior to 5 ng/ml TGF-β1 exposure. TRITC, tetramethylrhodamine isothiocyanate; DAPI, 4′,6-diamidino-2-phenylindole.

E-cadherin / α-SMA ; 

PubMed: 29207055     


Co-localization of E-cad and α-SMA occurs in A549 cells as determined by immunofluorescent staining. E-cad (green) was present in the cytoplasm, FITC-stained; α-SMA (red) was present in the cytoplasm, TRITC-stained. Cell nuclei were counterstained with DAPI (blue). Scale bar, 40 μm. The cell groups were as follows: control, cells cultured in serum-free DMEM; TGF-β1, cells cultured in serum-free DMEM and exposed to 5 ng/ml TGF-β1; SIS3, cells were treated with 3 μM SIS3 (specific inhibitor of Smad3) which was added 4 h prior to 5 ng/ml TGF-β1 exposure; BMSCs-CM, BMSCs-CM was added prior to 5 ng/ ml TGF-β1 exposure. E-cad, E-cadherin (E-calcium mucins); α-SMA, α-smooth muscle actin; TRITC, tetramethyl rhodamine isothiocyanate; FITC, fluorescein isothiocyanate; DAPI, 4′,6-diamidino-2-phenylindole.

29743238 25793924 29207055
体内研究 SIS3在Tie2-Cre;Loxp-EGFP小鼠中,抑制链脲霉素诱导的糖尿病性肾病中的Smad3激活。它还能减少AGE诱导的EndoMT、减少链脲霉素诱导的糖尿病性肾病中的EndoMT。SIS3在注射了链脲霉素的Tie2-Cre;Loxp-EGFP小鼠中,减少肾小球和肾小管间质中的IV型胶原以及纤连蛋白的表达。然而,SIS3并不减少蛋白尿[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: 正常人类皮肤成纤维细胞, 硬皮病成纤维细胞
  • Concentrations: 0.3, 1, 3 μM
  • Incubation Time: 72 h
  • Method:

    将正常人类皮肤成纤维细胞以105个细胞/孔的密度接种于6孔板中,以包含10%FCS的MEM培养基培养细胞,直到达到亚融合。将细胞培养在无血清的MEM培养基中24小时,然后加入(或不加入)SIS3,孵育72小时。用胰蛋白酶处理细胞,将细胞分离出来,进行计数。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: C57BL/6J雄性小鼠
  • Dosages: 1, 2.5或5 μg/g
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 97 mg/mL (197.96 mM)
Ethanol 24 mg/mL (48.98 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 489.99
化学式

C28H27N3O3.HCl

CAS号 521984-48-5
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03884621 Recruiting Other: EHP Group Stroke The Hong Kong Polytechnic University September 25 2018 Not Applicable
NCT02726685 Unknown status Other: respiratory training.|Other: sham training. Stroke Chung Shan Medical University August 1 2018 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID