S3I-201

For research use only. Not for use in humans.

目录号：S1155 别名： NSC 74859

CAS No. 501919-59-1

S3I-201 (NSC 74859) 有效抑制STAT3的DNA结合活性，IC50为86 μM，而对STAT1和STAT5的抑制活性低。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 638.93	现货
5mg	RMB 563.02	现货
10mg	RMB 972.36	现货
50mg	RMB 3028.28	现货
200mg	RMB 8165.43	现货
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客户使用Selleck生产的S3I-201发表文献165篇：

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Stem Cell Reports, 2017, 9(1):231-246

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Cell, 2017, 168(6):1053-1064

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Hepatology, 2017, 66(6):1934-1951

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Int J Cancer, 2016, 138(2):451-62

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Oncogene, 2016,

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Cancer Lett, 2016,

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产品安全说明书

STAT抑制剂选择性比较

生物活性

产品描述

S3I-201 (NSC 74859) 有效抑制STAT3的DNA结合活性，IC50为86 μM，而对STAT1和STAT5的抑制活性低。

特性

S3I-201是化学探测器抑制剂，可以除去乳腺瘤。

靶点

STAT3 ^[1]
(Cell-free assay)

86 μM

体外研究

S3I-201选择性抑制Stat3 DNA结合活性。S3I-201抑制Stat3·Stat3复合形式,不依赖于Stat3的激活状态。S3I-201不干涉Lck SH2与同源pTyr肽结合。S3I-201作用于NIH 3T3/v-Src鼠成纤维细胞和人类乳腺癌MDA-MB-231, MDA-MB-435, 和MDA-MB-468 细胞，可以抑制Stat3激活。S3I-201 抑制Stat3依赖的转录活性。 S3I-201 也抑制编码cyclin D1, Bcl-xL,和surviving 的Stat3-调节基因的表达。^[1]S3I-201可以降低 pS727STAT3水平和降低TGF-β通路蛋白水平。S3I-201也可抑制CD133+ 和CD133− Huh-7细胞。^[2]最新研究显示S3I-201作用于Hep-G2, Huh-7和SK-HEP-1细胞，加强 Cetuximab的抗增殖效果。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
U87	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MWm3NkBp		NW\ZSoZYUUN3ME21OU4yKM7:TR?=	M3fJclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEeyOlUzLz5{MEC3NlY2OjxxYU6=
U373	M1fDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYG3NkBp		M2rM[WlEPTB;NUKuOUDPxE1?	M4HIOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEeyOlUzLz5{MEC3NlY2OjxxYU6=
HPAC	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NHzJUlY4OiCq		M4DOTmlEPTExvK6xNFAh\|ryP	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB5Mk[1Nkc,OjByN{K2OVI9N2F-
PANC-1	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NWHq[VNjPzJiaB?=		MnO5TWM2OO,:nkGwNEDPxE1?	NFmwW4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO\|I3PTJ:L3G+
SK-BR-3	M4HsV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3vmc\|czKGh?		M1rmWWlEPTExvK6xNFAh\|ryP	MmXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByN{K2OVIoRjJyMEeyOlUzRC:jPh?=
U-373 MG	MY\DfZRwfG:6aXPpeJkhSXO\|YYm=	M4fXN\|MwOTBizszN	NGPPe2IzPCCq		M3zWbpJm\HWlZYOgSm4u\|rNvaX7keYNm\CClZXzsJI5mfXKxdH;4bYNqfHl?	M33KZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEi4OFE3Lz5{MEi4PFQyPjxxYU6=
MDA-MB-231	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M2m4dVczKGh?		M1ThXGlEPTExvK6xNFAh\|ryP	NVXkWIE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwO\|I3PTJpPkKwNFczPjV{PD;hQi=>
HUVEC	NIHmWlFHfW6ldHnvckBCe3OjeR?=	NGHXN3gxNjVvMkCg{txO	M3XnRlI1KGh?	NX\LVWh5TE2VTx?=	M2TUOJN2eHC{ZYPz[ZMhfGinIHj5dI95cWFvaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=>	Ml30QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3MkO1OVkoRjJzNUKzOVU6RC:jPh?=
Huh7	NFjtTXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFfZ[ogyODBibl2=	NIH0WVg1QCCq	M2PBb2ROW09?	M{nIPYlvcGmkaYTzJJRp\SCLTD22JJN1cW23bHH0bY9vKHC{b33veIVlKGOnbHygdJJwdGmoZYLheIlwdg>?	M13NSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{[0N\|g6Lz5{M{O2OFM5QTxxYU6=
PLC/PRF/5	NILGTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MW[xNFAhdk1?	MoWzOFghcA>?	MmrlSG1UVw>?	M3XGWIlvcGmkaYTzJJRp\SCLTD22JJN1cW23bHH0bY9vKHC{b33veIVlKGOnbHygdJJwdGmoZYLheIlwdg>?	NFW2cpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O2OFM5QSd-MkOzOlQ{QDl:L3G+
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MDA-MB-231	MoraRY51cXS3bX;yJIF{e2G7	NEjJSVU2KG2pL3vn	NGfMfHczKHenZXvz		MUfBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGW6cILld5NqdmdiYXP0bZZmKFO2YYSzJJhmdm:pcnHmeIVlKGmwIH3veZNmKGG2IEWgcYcwc2duIHn2JIZweiCndnXyfUA{KGSjeYOg[o9zKDJid3Xlb5M>	NVS2doJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0OlMxQTBpPkG3OFY{ODlyPD;hQi=>
NIH3T3	Ml7JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1TBPFExOCC3TR?=			M3[4e2dzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUDOWMzDj[YxteyCneIDy[ZN{cW6pII[tV5JkKGG2IEGwNEB2VSCob4Kg[ZZmenliMzDkZZl{KGK7IIPv[pQu[WejcjDjc4xwdnlvZn;ycYF1cW:wIHHzd4F6	MoDGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NkOwPVAoRjF5NE[zNFkxRC:jPh?=
A673	M3T5XZFJXFNiYYPzZZk>				MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	NX7DNpRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	M32wN5FJXFNiYYPzZZk>				NXfL[mg2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	NGTESXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	M3\JN5FJXFNiYYPzZZk>				NGPjNYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	MoHzdWhVWyCjc4PhfS=>				MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	M1LWd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	STAT3 / p-STAT3 / Cyclin D1 / Bcl-2 / Nanog / OCT4 / ALDH1 / CD44; PubMed: 26556875 Oncotarget Western blotting shows S3I-201 treatment decrease Cyclin D1, Bcl2 and self-renewal marker Nanog, OCT4, ALDH1, and CD44 in a dose dependent manner. Data shown are representative of three individual experiments. PD-L1; PubMed: 28605599 J Dent Res The expression level of PD-L1 was measured by Western blotting in a head and neck squamous cell carcinoma cell line (Cal 27 and FaDu), with and without S3I-201. β-Actin was used as the internal protein loading control. PD-L1, programmed death 1 ligand; STAT, signal transducers and activators of transcription; p-STAT3, phosphorylated STAT3.	26556875 28605599
Immunofluorescence	p-STAT3; PubMed: 26556875 Oncotarget Immunoflurosece shows S3I-201 reduce nuclear expression of p-STAT3Tyr705 by confocal microscope. Oct4 / Twist ; PubMed: 27521216 Oncotarget Suppression of Oct4 and Twist expression was shown in TW01 CD44/CD24 co-overexpressed cells and CSCs after S3I-201 treatment. Scale bars indicate 20 μm.	26556875 27521216
Growth inhibition assay	Cell viability; PubMed: 26813676 Blood The STAT3 inhibitor (S3I-201) decreases cellular proliferation in HTLV-I/ATL-lines. Cells were treated with 0, 12.5, 25, or 50 μM S3I-201 or dimethyl sulfoxide (DMSO) for 72 hours. The average growth curve is representative of the percentage of proliferation between S3I-201 and DMSO-treated cells. Each cell line was treated at least twice for standard deviation. 1185 (-IL2) cells were washed in phosphate-buffered saline and resuspended in media without IL2, followed by treatment with S3I-201 for 72 hours.	26813676

体内研究

5 mg/kg剂量的S3I-201作用于携带人类乳腺癌(MDA-MB-231)的鼠时，显示出强抑制效果。^[1]5 mg/kg剂量的S3I-201作用于Huh-7移植瘤，显示出强抗癌活性，没有明显的外部健康改变或者体重减轻症状。^[2]

激酶实验：^[1]	- 合并体外Stat3 DNA结合实验和EMSA分析: 100 mL生物素-e-Ac-EPQpYEEIEL-OH (溶于50 mM Tris/150 mM NaCl, pH 为7.5) 加到链霉亲和素包被的96孔微型板的每孔中，在4^oC下振荡温育过夜。用PBS/Tween-20冲洗板，然后加入2次200 mL BSA-T-PBS (0.2% BSA/0.1% Tween-20/PBS)。50 mL Lck-SH2-GST 融合蛋白(6.4 ng/ml，溶于BSA-T-PBS中)加到96孔板的每孔中，在室温下振荡处理4小时。转移溶液，用200 mL BSA-T-PBS冲洗4次,然后在每孔中加入100 mL多克隆GST抗体 (100 ng/mL，溶于BSA-T-PBS)，4^oC下温育过夜。用BSA-T-PBS冲洗后, 在每孔中加入100 mL 200 ng/ml BSA-T-PBS辣根过氧化物酶结合的二抗，然后在室温下温育45分钟。用BSA-T-PBS冲洗4步后，再用PBS-T冲洗3步，然后在每孔中加入100 mL过氧化物酶底物，温育5到15分钟。加入100 mL 1 M硫酸溶液终止过氧化物酶反应，使用ELISA计数板在450nm 处读取吸光值。
细胞实验：^[2]	- 合并 Cell lines: HCC细胞系包括HepG2, PLC/PRF/5, SNU-449, Huh-7, SNU-398, SNU-182，和SNU-475 Concentrations: 25到250 μM Incubation Time: 72小时 Method: 5 ×10³个细胞接种在含完全培养基的96孔微型板上。培养72小时后，每孔加入100 μL 2 mg/mL MTT溶液测量存活细胞数。2小时后，转移培养基，每孔加入100 μL二甲亚砜溶解甲结晶。使用酶联免疫吸附法计数器在590 nm处读取吸光值。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 6周大的携带MDA-MB-231移植瘤模型的雌性无胸腺裸鼠 Dosages: 5 mg/kg Administration: 静脉注射，每周2天或3天。 (Only for Reference)

参考文献

[4] Sen N, et al. Proc Natl Acad Sci U S A, 2012, 109(2), 600-605.

- 合并

溶解度 (25°C)

体外	DMSO	73 mg/mL (199.8 mM)
	Water	Insoluble
	Ethanol	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)： 5% DMSO+corn oil	3mg/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 Download S3I-201 SDF

分子量	365.36
化学式	C₁₆H₁₅NO₇S
CAS号	501919-59-1
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	NSC 74859

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

每只动物给药体积

动物数量

只

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

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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、SDS / 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

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、SDS / 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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

研究领域

产品类型

定制您的化合物库

S3I-201

客户使用Selleck生产的S3I-201发表文献165篇：

产品安全说明书

STAT抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download S3I-201 SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

技术支持

STAT Signaling Pathway Map

相关STAT产品