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。

规格 价格 库存 购买数量  
In DMSO RMB 1171.35 现货
RMB 896.27 现货
RMB 3834.82 现货
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客户使用Selleck该产品发表文献231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 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 MoOxSpVv[3Srb36gRZN{[Xl? MV2xNEDPxE1? M2fVd|IzKGh? NIDPZnVFVVOR M3\yfGlvcGmkaYTzJHRISlJ{IIPp[45idGmwZzDpckBpfW2jbjDISWszQTOWIHPlcIx{KGG|c3Xzd4VlKGG|IFnubIljcXSrb36gc4YhW02DRDDhZ5RqfmG2aX;uJJdqfGhiSVO1NEBw\iByLkC2Ou69VQ>? M{WzXFI{OTNyNkK2
H1299 Mn31UYloemG2aX;uJGF{e2G7 MUWxJO69VQ>? NEPQXJIyOi1{NDDo MYPEUXNQ M3n2Xmlv\HWlZYOgZY51cW2rZ4LheI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGgyOjl7IHPlcIx{KGG|c3Xzd4VlKGG|IFnubIljcXSrb36gc4Yh[2WubDDtbYdz[XSrb36ge4l1cCCLQ{WwJI9nKDBwNd88US=> NVTa[IN1OjR2MUe0O|k>
HaCaT NED3bopHfW6ldHnvckBCe3OjeR?= NIX5XFI{NjJvNUCg{txO MUSxOUBucW5? NY[1eZpSTE2VTx?= NH76PZNKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>? M3\ndFIxQTF7Nke4
HepG2 Ml7ZSpVv[3Srb36gRZN{[Xl? MWKxNkBp NXzqWWZMTE2VTx?= NEjBSY1KdmirYnn0d{BVT0[ULUGgbY4hcHWvYX6gTIVxTzJiY3XscJMh\XiycnXzd4lv\yCSQVmtcJVkcW[ncnHz[UB4cXSqIFnDOVAhd2ZiMD6yOe69VQ>? NH;5U5gyQTlzNEC2PC=>
CHO-HIR M1fvdmZ2dmO2aX;uJGF{e2G7 Mlj4NE4xOS1|IN88US=> M1fOSVIhcA>? MoX2SG1UVw>? M4q3fGlvcGmkaYTzJHRITmKndHGtbY5lfWOnZDDkc5dve3S{ZXHtJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKEGOS{Wg[ZhxemW|c3XkJIlvKEOKTz3ITXIh[2WubIOgZZN{\XO|ZXSgZZMhcW62cnHj[YxtfWyjcjD0doFve2yxY3H0bY9vKG:oIFXHSnAuW22jZEKge4l1cCCLQ{WwJI9nKDBwM{ZOwG0> Mn\jNlQxPTVyNE[=
Sf9 MVHGeY5kfGmxbjDBd5NigQ>? M4LyNlIhcA>? NIXKTmVFVVOR M4PL[GlvcGmkaYTzJIh2dWGwIILlZ49u[mmwYX70JGFNUzVicHjvd5Bpd3K7bHH0bY9vKGW6cILld5Nm\CCrbjDT[lkh[2WubIOge4l1cCCLQ{WwJI9nKDFwNUSy{txO MkjsNVc2PTJ3MEe=
C32 Mn7GSpVv[3Srb36gRZN{[Xl? MnTINVAh|ryP M2XVXVIxcA>? M3\k[2lvcGmkaYTzJHRzgXCjbn;zc41iKGO{dYrpJHkhcW6oZXP0bY9vNWmwZIXj[YQhXEeIYnX0ZUB{cWewYXzpcochcW5ibXnub{BEOzJiY3XscJMh[XRiMUCgeW0> M3fsc|E4PTJ4N{W3
Mouse embryo cardiomyocytes MX7GeY5kfGmxbjDBd5NigQ>? MoLTNVAh|ryP MoS4NUBp NVPueY5SUW6qaXLpeJMhcW64YYPpc44hd2ZiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDlcYJzgW9iY3Hy[IlwdXmxY4n0[ZMh[XO|ZYPz[YQh[XNicHH0bI9o\W5iaX7m[YN1cW:wIHH0JFExKHWP NW\1fpVsOTd3Mk[3OVc>
Mouse embryo cardiomyocytes M{f6XmZ2dmO2aX;uJGF{e2G7 NHfPc5EyOCEQvF2= MojUNUBp NFzhc5JKdmirYnn0d{BVT0ZvYnX0ZU0yNWmwZIXj[YQhW22jZEKgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIHXtZpJ6dyClYYLkbY9ugW:leYTld{BifCBzMDD1US=> M1fQb|E4PTJ4N{W3
Mouse embryo cardiomyocytes NFLGVJVHfW6ldHnvckBCe3OjeR?= M3nsPFExKM7:TR?= NIrOfZoyKGh? MU\Jcohq[mm2czDUdplx[W6xc3;tZUBkenW8aTDEcVI5SyCrbn\lZ5Rqd25vaX7keYNm\CCVbXHkNkBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3Wg[Y1jenmxIHPhdoRqd227b3P5eIV{KGG2IEGwJJVO NFj0Xo0yPzV{Nke1Oy=>
Trypanosoma cruzi trypomastigotes MYDBcpRqdWmlcn;ibYFtKEG|c3H5 MYSxNEDPxE1? M3nR[lQhcA>? NGr5To1KdmS3Y3XzJIFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBkenW8aTD0dplxd22jc4Tp[491\XNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJJBiemG|aYTlJI1wenCqb3zv[5kh[XRiMUCgeW0> MUmxO|UzPjd3Nx?=
Mouse cardiomyocytes NV\xRYNJSW62aX3pZ5Jw[mmjbDDBd5NigQ>? MkjWNVAh|ryP M4X1NlQhcA>? M1flfWlv\HWlZYOgZY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTDh[4FqdnO2IGTyfZBidm:|b33hJINzfXqrIGmgbY4hdW:3c3WgZ4Fz\GmxbYnvZ5l1\XNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGmwdILhZ4VtdHWuYYKgZY1ie3SrZ3;0[ZMh[XRiMUCgeW0> MUixO|UzPjd3Nx?=
Mouse cardiomyocytes MYHBcpRqdWmlcn;ibYFtKEG|c3H5 MYSxNEDPxE1? MnzFPVYhcA>? MXTJcoR2[2W|IHHueIl1enmyYX7vd49u[WxiYXP0bZZqfHliYXfhbY5{fCCWconwZY5we2:vYTDjdpV7cSC\IHnuJI1wfXOnIHPhdoRqd227b3P5eIV{KGG|c3Xzd4VlKGG|IFnubIljcXSrb36gc4YhfHK7cH;tZZN1cWexdHWgdoVt\WG|ZTDheEAyOCC3TR?= M3r6N|E4PTJ4N{W3
HaCaT M3TITGZ2dmO2aX;uJGF{e2G7 MlztNE4xPSEQvF2= NFW3bpIzKGh? MlPESG1UVw>? M4S3ZmRw\XNibn;0JIlvcGmkaYSgWGdHNWKndHGgbY5lfWOnZDDBUGs2KGGldHn2bZR6KGmwIFjhR4FVKGOnbHzzJIF{e2W|c3XkJIF{KHB|VGCtcJVkcW[ncnHz[UBz\XCxcoTldkBi[3Srdnn0fUBifCByLkC1JJVO NULXdGZVOTd3NUK1NFc>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phospho-SMAD3 / Phospho-p38 ; 

PubMed: 17113264     


Quiescent IMR-90 cells were treated with/without TGF-β1 (2 ng/ml) in the presence or absence of increasing concentrations of the TGF-βR1(ALK5) inhibitor, SB431542. Cell lysates were collected after 45 min and assessed by SDS-PAGE followed by western immunoblotting for phospho-SMAD3 and phospho-p38 MAPK. The blots were then striped and probed for total SMAD3 and p38 MAPK, respectively.

Y397 phospho-FAK; 

PubMed: 17113264     


Quiescent IMR-90 cells were treated with TGF-β1 (2 ng/ml) in the presence/absence of the p38 MAPK inhibitor, SB203580 (6 μM). Cell lysates collected after 16 h were assessed for Y397-phosphorylated FAK by SDS-PAGE and western immunoblotting. Blots were stripped and probed for total FAK.

pSmad2 / p-AKT / E-cadherin / vimentin / snail / slug; 

PubMed: 26269769     


B16-pldMock cells and B16-pldNodal cells were treating with SB431542 (10 mM) in a time dependent manner, and then the protein was collected for Western blotting analysis.

CK18 / Fibronectin / Vimentin; 

PubMed: 30134011     


Representative Western blots (upper panel) and densitometric analysis (lower panel) for E‐cadherin, CK18 (epithelial markers), fibronectin and vimentin (mesenchymal markers) normalized to β-actin in HepG2 and BEL7402 cells with or without SB431542 treatment in CM and HBSS.

17113264 26269769 30134011
Growth inhibition assay
Cell viability; 

PubMed: 28125630     


Cells were treated with 1 mg/L, 4 mg/L, and 16 mg/L of fluoride with or without 10μmol/L SB431542 for 4 and 7 days. MTT assay was used to detect cell viability. Absorbance was measured at 490 nm in aspectrophotometer. Average optical density (OD) value of cells viability was represented as mean±SD (n = 8) (*P < 0.05, **P < 0.01 compare with control group; aa P< 0.05, compare with SB431542 group).

28125630
Immunofluorescence
Smad2/3; 

PubMed: 19619490     


MEFs were treated with 25 mM glucose, TGF-β or glucose and SB431542 for 30 min, and the subcellular localization of Smad2/3 was visualized. DAPI was used to stain the nuclei.

19619490
Immunofluorescence
Na+/K+-ATPase; 

PubMed: 23451286     


Blocking the TGF-receptor signaling by SB431542 enabled the subcellular localization of Na+/K+-ATPase and ZO-1 at the plasma membrane. Scale bar: 100 μm.

23451286
ELISA
collagen 1; 

PubMed: 23451286     


ELISA assay revealed that SB431542 significantly downregulated the secretion of type I collagen to the culture supernatant. **P<0.05.

23451286
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]
- 合并

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]
- 合并
  • 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]
- 合并
  • 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
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

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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