SIS3 HCl

目录号：S7959

SIS3 HCl Chemical Structure

Molecular Weight(MW): 489.99

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。

规格 价格 库存 购买数量  
RMB 795.17 现货
RMB 1204.05 现货
RMB 3661.13 现货
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客户使用Selleck该产品发表文献18篇：

客户使用该产品的5个实验数据：

  • Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, *P<0.05, **P<0.01.

    Circ Res, 2017, 121(6):617-627. SIS3 HCl purchased from Selleck.

  • Levels of PAI-1, phosphorylated SMAD3 at s425 as well as total SMAD3 were determined with western blot in 95D and A549 NSCLC cells after treatment with TGF-β and SIS3.

    Cell Physiol Biochem, 2017, 44(6):2201-2211. SIS3 HCl purchased from Selleck.

  • Effect of SIS3, Smad3 inhibitor on TMAO-induced Cardiac Hypertrophy. SIS3 (3 μM) was used to treat cardiomyocytes in the presence or absence of TMAO for 72 h. The cell areas were detected by an immunofluorescence assay in neonatal mouse cardiomyocytes (Scale bar: 25 µm).

    Lab Invest, 2018, doi: 10.1038/s41374-018-0091-y. SIS3 HCl purchased from Selleck.

  • SIS3 alleviates BLM-induced lung fibrosis. Mice were intratracheally challenged with BLM (1.5 mg/kg) or saline on day 0, and with either SIS3 or control vehicle by intraperitoneal injection (2 mg/kg) every other day until the end of the experiment. Mice were sacrificed three weeks after BLM challenge. (A) Lung morphology of mice in each group was evaluated by hematoxylin-eosin staining. (B) Collagen fiber deposition in pulmonary interstitium was evaluated by Masson's staining in lungs in rats of each group. Ashcroft score (C) and hydroxyproline content (D) on day 21 after BLM administration. Results are expressed as means ±SD (n ¼ 5). Statistical analysis of indicated columns was performed using Student's t-test. **P < 0.01. ***P < 0.001.

    Biochem Biophys Res Commun, 2018, 503(2):757-762. SIS3 HCl purchased from Selleck.

  • Fibroblasts were pretreated with SIS3 for 1 hour and then incubated with 10 ng/mL TGF-b1 for 24 hours. Whole-cell lysates were examined by Western blot analysis. TGF-b1-induced Tnc expression was significantly abrogated by SIS3 (SIS3 diluted in DMSO, 3 μM) (***P <.001, **P <.01). Tnc = tenascin-C.

    Laryngoscope, 2018, doi: 10.1002/lary.27164. SIS3 HCl purchased from Selleck.

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 MXXD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NFz5ZXM26oDLzszN NIrseWcyKGh? NYH5PVk1XHKnYYTt[Y51KHerdHigV2lUOyC|dYDwdoV{e2WmIHPh[I1qfW1vaX7keYNm\CCKSz2yJINmdGxiZHXheIgv MWizNFgxPDR5MB?=
A549 cells NUPxe3p4TnWwY4Tpc44h[XO|YYm= M4LaW|Mh|ryP NXfxPJdJXGinIHPlcIx{KGmwIITo[UBUUVN|IHfyc5VxKGSrc4DsZZlm\CCjIIPwbY5ldGVvc3jhdIVlKGWub37nZZRm\CCoaXLyc4Jt[XO2LXzpb4UhdW:{cHjvcI9ogS5? MnjaNlkzODdyNUW=
AML12 cell line M2TmNGZ2dmO2aX;uJIF{e2G7 MVmxNEDPxE1? NYLiOoJ2OzBibXnudy=> NXizUndPW0mVMzDicI9kc3NiVFfGMe6zNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVTVHEN{BidmRidHjlJJRwfGGuIGPNRWQzNzNibHX2[Yx{KGG{ZTD1coNp[W6pZXSu MljhNlc1PjJyN{W=
A549 cells NIH1S29HfW6ldHnvckBie3OjeR?= NXz1bYNwOyEQvF2= MnPzOEBp MkDjV2lUOyC|aXfubYZq[2GwdHz5JJJme3SxcnXkJGUu[2GmaHXybY4h\XiycnXzd4lwdiCjbnSgbY1x[Wm{ZXSgeolu\W62aX6gZY5lKFOwYXnsJIV5eHKnc4Ppc44hcW5idHjlJJBz\XOnbnPlJI9nKFSJRj5OtlEv M36xZ|I1PTd|MEO4
MCF-7 cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 NEHvfIszNjVizszN MXfjc45kfXK{ZX70JJRz\WG2bXXueEB4cXSqIGPJV|MhemWmdXPl[EB1cGViaX7obYJqfG:{eTDl[oZm[3Rib3[g[Yxt[WerYzDhZ4llKG:wIITo[UBxem:uaX\ldoF1cW:wIH;mJG1ETi15IHLy[YF{fCClYX7j[ZIh[2WubIOu NX;XWVlyOjR3MkiwN|g>

... 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
  • Formulation: --
  • 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

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 Not yet recruiting 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