SB431542

目录号:S1067

SB431542 Chemical Structure

Molecular Weight(MW): 384.39

SB431542是一种有效的,选择性ALK5抑制剂,无细胞试验中IC50为94 nM,对ALK5的作用比对p38、MAPK和其他激酶强100倍。

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RMB 1171.35 现货
RMB 896.27 现货
RMB 3834.82 现货
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客户使用该产品的10个实验数据:

  • Phase-contrast images of RPBJ- and HNF6-deficient hepatocyte spheroids embedded in collagen gels and cultured in the presence or absence of the TGFβ inhibitor SB-431542 (SB) for the indicated number of days.

    Nature, 2018, 557(7704):247-251. SB431542 purchased from Selleck.

    Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01.

    Acta Biomater 2014 10(7):3108-16. SB431542 purchased from Selleck.

  •  

    Hedgehog, Igf and Tgf signaling are required for myocardial regeneration in zebrafish. (C) Quantification of the effects of CyA (10 uM), NVP AEW541 (2 uM) and SB-431542 (10 uM) on cardiomyocyte proliferation after resection injury. Fish were treated from 6 to 7 dpa. (D) Quantification of the effects of CyA, NVP AEW541 and SB-431542 on proliferation after genetic cardiomyocyte ablation.

    Development 2013 140, 660-666. SB431542 purchased from Selleck.

    Transforming growth factor-b (TGF-b)/Smad3 induces Akt phosphorylation in vascular smooth muscle cells (SMCs). C: vascular SMCs were pretreated with the TGF- receptor inhibitor SB431542 (10 uM) for 30 min and then stimulated with TGF- (5 ng/ml) for 12 h, and p-Akt was measured by Western blot analysis.

    Am J Physiol Heart Circ Physiol 2012 302, H2211-H2219. SB431542 purchased from Selleck.

  •  

    Effect of small molecule inhibitors on reprogramming efficiency of myoblast cell derived from 5 different donors. (A) Reprogramming efficiency is shown as number of colonies from 10^5 starting cells on Y-axes. Ctrl, control condition and addition of small molecule inhibitors are marked. (B) AP staining of reprogrammed myoblast cell lines, from 5 different donors, in wells of 12-well plates at day 18. Ctrl, control condition and additions of small molecule inhibitors are marked.

    Stem Cells Dev 2013 SB431542 purchased from Selleck.

    Retroviral reprogramming of myoblasts. (C) Small molecule inhibitors effect on reprogramming efficiency compared to control. (D) AP staining of reprogrammed plates with or without inhibitors. Close-up of AP staining, bar 500 um; AP, alkaline phosphatase.

    Stem Cells Dev 2013 SB431542 purchased from Selleck.

  •  

    TGFb1 mRNA expression in different follicles of the 26 weeks old hen ovaries and its effect on CTGF mRNA expression in granulosa cells. Effects of TGFb1 and inhibitor SB431542 on CTGF mRNA expression in granulosa cells from F2 to F4 and POF1 follicles.

    Gen Comp Endocr 2012 178, 314–322. SB431542 purchased from Selleck.

    SB431542 inhibit expression of TGF-beta induced pS2 in MvILu cell

     

     

    Dr. Kah-Wai Lin of Karolinska Biomics Center. SB431542 purchased from Selleck.

  • SB431542 purchased from Selleck.

    (C) C3H10T1/2 cells transfected with pEF-BOS or pEF-Flag-TAZ were cultured for 8 days in osteogenic medium (OM) including ascorbic acid and β-glycerophosphate in the absence or presence of TGF-β inhibitors (SB-431542 or SB-525334). ALP activity was measured in the cell layer and normalized to cellular protein content. Data are expressed as means 6 ± SD ( *p < 0.05 vs. pEF-BOS, # p < 0.01 vs. vehicle) (D) Quantitative RT-PCR analysis of Col 1 and ALP in C3H10T1/2 cells.

    SB431542 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 SB431542是一种有效的,选择性ALK5抑制剂,无细胞试验中IC50为94 nM,对ALK5的作用比对p38、MAPK和其他激酶强100倍。
特性 SB-431542在EGFR激酶域引起点突变,或上调HER3下游信号通路。
靶点
ALK4 [2]
(Cell-free assay)
ALK7 [2]
(Cell-free assay)
ALK5 [1]
(Cell-free assay)
94 nM
体外研究

SB-431542作用于A498细胞无细胞毒性,LD50大于30 μM。[1] SB-431542也抑制ALK4和ALK7,这两种含有磷酸化Smad2。SB-431542对ALK1, ALK2, ALK3,和ALK6抑制作用不大, 这四种含磷酸化Smad1。SB-431542选择性抑制内生的活化素,而对BMP信号没有作用效果。SB-431542可以诱导Smad2/Smad4和Smad3/Smad4依赖的转录。[2] 在A498细胞中, SB-431542抑制TGF-β1诱导的胶原Iα1 和PAI-1 mRNA,IC50分别为60和50 nM。此外,SB-431542抑制TGF-β1诱导的纤连蛋白mRNA和蛋白,IC50分别为62和22 nM。 [3]SB-431542抑制TGF-β调节的生长因子,包括PDGF-A, FGF-2 和HB-EGF, 可以增强MG63细胞增殖。SB-431542也抑制TGF-β诱导的 c-Myc和p21WAF1/CIP1。[4] 在FET, RIE, 和Mv1Lu细胞中,SB-431542 明显抑制TGF-β诱导的G1 期阻滞,且SB-431542诱导细胞周期S期细胞数累积。在NMuMG和PANC-1细胞中,SB-431542也抑制TGF-β调节的上皮细胞向间质转型(EMT)。[5] SB-431542通过人类DC的功能成熟和IL-12产生而诱导NK活性。[6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T M1LrfWZ2dmO2aX;uJGF{e2G7 MnTkNVAh|ryP M2\PNFIzKGh? NV\UfVNWTE2VTx?= MYrJcohq[mm2czDUS2JTOiC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCLbnjpZol1cW:wIH;mJHNOSURiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yNkdOwG0> M3z5clI{OTNyNkK2
H1299 NVntS4NHVWmpcnH0bY9vKEG|c3H5 MoLXNUDPxE1? MkXKNVIuOjRiaB?= NVTaPJo5TE2VTx?= M2fOVGlv\HWlZYOgZY51cW2rZ4LheI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGgyOjl7IHPlcIx{KGG|c3Xzd4VlKGG|IFnubIljcXSrb36gc4Yh[2WubDDtbYdz[XSrb36ge4l1cCCLQ{WwJI9nKDBwNd88US=> MX[yOFQyPzR5OR?=
HaCaT MYrGeY5kfGmxbjDBd5NigQ>? MXezMlIuPTBizszN NH\xVWkyPSCvaX6= M33RU2ROW09? NWHaVHYzUW6qaXLpeJMhXEeIYnX0ZUBz\WOncITvdkBqdiCqdX3hckBJ[UOjVDDj[YxteyCjc4Pld5Nm\CCjczDTcYFlKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6xO|LPxE1? NI\NfpkzODlzOU[3PC=>
HepG2 MXXGeY5kfGmxbjDBd5NigQ>? NFHNNZgyOiCq MmjRSG1UVw>? M3r2VWlvcGmkaYTzJHRITlJvMTDpckBpfW2jbjDI[ZBIOiClZXzsd{BmgHC{ZYPzbY5oKFCDST3seYNq\mW{YYPlJJdqfGhiSVO1NEBw\iByLkK1{txO NY\tWIlCOTl7MUSwOlg>
CHO-HIR NHnHTopHfW6ldHnvckBCe3OjeR?= NXTzR5U{OC5yMT2zJO69VQ>? NYPSNGFoOiCq NFjYS2VFVVOR NF63d49KdmirYnn0d{BVT0[kZYThMYlv\HWlZXSg[I94dnO2cnXhcUB1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBw\iCDTFu1JIV5eHKnc4Pl[EBqdiCFSF:tTGlTKGOnbHzzJIF{e2W|c3XkJIF{KGmwdILhZ4VtdHWuYYKgeJJidnOub3PheIlwdiCxZjDFS2ZRNVOvYXSyJJdqfGhiSVO1NEBw\iByLkO1{txO MX[yOFA2PTB2Nh?=
Sf9 MoroSpVv[3Srb36gRZN{[Xl? M4\LOVIhcA>? NXXIZoJ2TE2VTx?= NVTKTXM5UW6qaXLpeJMhcHWvYX6gdoVkd22kaX7hcpQhSUyNNTDwbI9{eGixconsZZRqd25iZYjwdoV{e2WmIHnuJHNnQSClZXzsd{B4cXSqIFnDOVAhd2ZiMT61OFLPxE1? NWPFcGhUOTd3NUK1NFc>
C32 MUTGeY5kfGmxbjDBd5NigQ>? NFXlfZEyOCEQvF2= NGm5U|gzOGh? MV3Jcohq[mm2czDUdplx[W6xc3;tZUBkenW8aTDZJIlv\mWldHnvck1qdmS3Y3XkJHRITmKndHGgd4lodmGuaX7nJIlvKG2rbnugR|MzKGOnbHzzJIF1KDFyIIXN NWXs[pZnOTd3Mk[3OVc>
Mouse embryo cardiomyocytes MUjGeY5kfGmxbjDBd5NigQ>? Mlm3NVAh|ryP NXXv[XF2OSCq M1zhNWlvcGmkaYTzJIlvfmG|aX;uJI9nKFS{eYDhco9{d22jIHPyeZpqKFliaX6gcY92e2ViZX3idplwKGOjcnTpc416d2O7dHXzJIF{e2W|c3XkJIF{KHCjdHjv[4VvKGmwZnXjeIlwdiCjdDCxNEB2VQ>? NX:3RYNoOTd3Mk[3OVc>
Mouse embryo cardiomyocytes NUPDbZFMTnWwY4Tpc44hSXO|YYm= MY[xNEDPxE1? MoH0NUBp NWXMelJ4UW6qaXLpeJMhXEeILXLleIEuOS2rbnT1Z4VlKFOvYXSyJJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDlcYJzgW9iY3Hy[IlwdXmxY4n0[ZMh[XRiMUCgeW0> NESy[JMyPzV{Nke1Oy=>
Mouse embryo cardiomyocytes MXPGeY5kfGmxbjDBd5NigQ>? NGDS[GoyOCEQvF2= NX7G[G42OSCq MXjJcohq[mm2czDUdplx[W6xc3;tZUBkenW8aTDEcVI5SyCrbn\lZ5Rqd25vaX7keYNm\CCVbXHkNkBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3Wg[Y1jenmxIHPhdoRqd227b3P5eIV{KGG2IEGwJJVO MUmxO|UzPjd3Nx?=
Trypanosoma cruzi trypomastigotes NUS4T|lSSW62aX3pZ5Jw[mmjbDDBd5NigQ>? NWP3fJJ7OTBizszN NWHZUGhwPCCq M3K0SWlv\HWlZYOgZY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTDh[4FqdnO2IGTyfZBidm:|b33hJINzfXqrIITyfZBwdWG|dHnnc5RmeyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gdIFz[XOrdHWgcY9zeGixbH;nfUBifCBzMDD1US=> M1v0R|E4PTJ4N{W3
Mouse cardiomyocytes MkjVRY51cW2rY4LvZolidCCDc4PhfS=> NV7UTYxEOTBizszN NFXmdFQ1KGh? M{P6VGlv\HWlZYOgZY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTDh[4FqdnO2IGTyfZBidm:|b33hJINzfXqrIGmgbY4hdW:3c3WgZ4Fz\GmxbYnvZ5l1\XNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGmwdILhZ4VtdHWuYYKgZY1ie3SrZ3;0[ZMh[XRiMUCgeW0> M4LrTlE4PTJ4N{W3
Mouse cardiomyocytes NXnMeXE3SW62aX3pZ5Jw[mmjbDDBd5NigQ>? MXqxNEDPxE1? NVXKcmVnQTZiaB?= NGGxT4dKdmS3Y3XzJIFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBkenW8aTDZJIlvKG2xdYPlJINiemSrb335c4N6fGW|IHHzd4V{e2WmIHHzJGlvcGmkaYTpc44hd2ZidIL5dI9u[XO2aXfveIUhemWuZXHz[UBifCBzMDD1US=> MVSxO|UzPjd3Nx?=
HaCaT NXm1NIpDTnWwY4Tpc44hSXO|YYm= NU\XVWNWOC5yNTFOwG0> M36wN|IhcA>? NVzJfmFETE2VTx?= M1\lU2Rw\XNibn;0JIlvcGmkaYSgWGdHNWKndHGgbY5lfWOnZDDBUGs2KGGldHn2bZR6KGmwIFjhR4FVKGOnbHzzJIF{e2W|c3XkJIF{KHB|VGCtcJVkcW[ncnHz[UBz\XCxcoTldkBi[3Srdnn0fUBifCByLkC1JJVO MljMNVc2PTJ3MEe=

... Click to View More Cell Line Experimental Data

体内研究 在结肠癌模型中,SB-431542导致 毒性T淋巴细胞激活 (CTL) ,且通过TGF-ß 抑制的DC功能改变,产生抗癌免疫效果。[6]

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)

激酶实验:[1]
+ 展开

激酶实验:

SB-431542溶解在DMSO中,浓度为10 mM。在杆状病毒表达系统中,TGFβRI的激酶域,:第200号氨基酸到C-端,和全长Smad3蛋白表达作为 N-端谷胱甘肽S转移酶(GST)融合蛋白。加入谷胱甘肽凝胶来纯化蛋白。用0.1 M 无菌过滤的碳酸氢钠(pH 为7.6)包被FlashPlates,每100 μL中加入700 ng GST-Smad3。实验buffer包含50 mM HEPES (pH 为7.4), 5 mM MgCl2, 1 mM CaCl2, 1 mM DTT, 100 mM GTP, 3 μM ATP,0.5 μCi/孔33P-ATP, 及85 ng GST-ALK5。 在30oC下温育3小时。在Packard TopCount 96孔闪烁计数器上读数。
细胞实验:[1]
+ 展开
  • Cell lines: A498细胞
  • Concentrations: 100 μM 左右
  • Incubation Time: 48小时
  • Method: A498细胞按每孔5-10×103个接种在96孔板上。细胞血清饥饿处理24小时,然后用SB431542处理48小时,测定细胞毒性。然后加入XTT标签和细胞温育4小时,测定细胞活力。
    (Only for Reference)
动物实验:[6]
+ 展开
  • Animal Models: 腹腔注射结肠-26肿瘤细胞的BALB/c鼠
  • Formulation: 溶于0.1 % DMSO
  • Dosages: 1 μM 溶液, 100 μL/鼠
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 76 mg/mL (197.71 mM)
Ethanol 3 mg/mL (7.8 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+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 384.39
化学式

C22H16N4O3

CAS号 301836-41-9
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    I would appreciate it if you can help me in figuring out the formulation for this drug in vivo experiments.

  • 回答:

    S1067 SB431542 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension for oral gavage. It can also be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml as a clear solution for IP injection.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID