NSC 74859 (S3I-201)

目录号：S1155 Purity: 99.28%

NSC 74859 (S3I-201)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。

NSC 74859 (S3I-201) Chemical Structure

CAS: 501919-59-1

规格	价格	库存
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
1g	RMB 22113	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的NSC 74859 (S3I-201)发表文献220篇

产品质控

批次：纯度： 99.28%

99.28

NSC 74859 (S3I-201)相关产品

相关靶点	STAT1 STAT3 STAT5 STAT6	点击展开
相关化合物库	激酶抑制剂库 FDA药物库天然产物库酪氨酸激酶抑制剂分子库 JAK-STAT信号通路库	点击展开

STAT抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
H1299	Function Assay	50/100 μM	48 h	suppresses miR-92a expression dose-dependently	23820254
H460	Function Assay	50/100 μM	48 h	inhibits the Stat3C increased miR-92a expression	23820254
PLC/PRF/5	Growth Inhibition Assay	100 nM	48 h	inhibits the IL-6 stimulation promoted cell proliferation	23364389
Huh7	Growth Inhibition Assay	100 nM	48 h	inhibits the IL-6 stimulation promoted cell proliferation	23364389
HUVEC	Function Assay	0.5-20 μM	24 h	suppresses the hypoxia-induced accumulation of HIF-1α	21523559
U-373 MG	Cytotoxicity Assay	3/10 μM	24 h	reduces FN-γ-induced cell neurotoxicity	20888416
U373	Growth Inhibition Assay	125 μM	24 h	disrupts STAT3 signaling and proliferation	24070820
HUT-102	Apoptosis Assay	75-300 μM	24/48 h	suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis	24090995
MT-2	Apoptosis Assay	75-300 μM	24/48 h	suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis	24090995
H460	Apoptosis Assay	100 nM	24 h	enhances cell death co-treated with LY294002	24472538
A459	Apoptosis Assay	100 nM	24 h	induces cell apoptosis co-treated with BEZ235	24472538
H460	Apoptosis Assay	100 nM	24 h	induces cell apoptosis co-treated with BEZ235	24472538
GC	Growth Inhibition Assay	50-125 μM	72 h	attenuates the cell growth in a dose-dependent manner	25774503
GH3	Growth Inhibition Assay	50-125 μM	72 h	attenuates the cell growth in a dose-dependent manner	25774503
BT474R	Function Assay	50 μM	10-60 d	inhibits STAT3 activity	25327561
NCI-N87R	Function Assay	50 μM	10-60 d	inhibits STAT3 activity	25327561
MDA-MB-468	Function assay	100 uM	24 hrs	Inhibition of Stat3 activation in human MDA-MB-468 cells at 100 uM after 24 hrs	17463090
MDA-MB-435	Function assay	100 uM	24 hrs	Inhibition of Stat3 activation in human MDA-MB-435 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Function assay	100 uM	24 hrs	Inhibition of Stat3 activation in human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
NIH3T3	Function assay	100 uM	24 hrs	Reduction of pTyr-705 Stat3 level in v-Src expressing mouse NIH3T3 cells at 100 uM after 24 hrs	17463090
NIH3T3	Growth inhibition assay	100 uM	4 days	Growth inhibition of mouse NIH3T3 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-435	Growth inhibition assay	100 uM	4 days	Growth inhibition of human MDA-MB-435 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-231	Growth inhibition assay	100 uM	4 days	Growth inhibition of human MDA-MB-231 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-468	Growth inhibition assay	100 uM	4 days	Growth inhibition of human MDA-MB-468 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-435	Apoptosis assay	30 to 100 uM	48 hrs	Induction of apoptosis in human MDA-MB-435 cells expressing active Stat3 at 30 to 100 uM after 48 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs	Reduction of apoptosis in Stat3 transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs	Reduction of cyclin D1 gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs	Induction of apoptosis in Stat3 SH2 domain transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs	Induction of apoptosis in Stat3C transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs	Reduction of cyclin D1 gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs	Reduction of Bcl-xL gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs	Reduction of survivin gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs	Reduction of Bcl-xL gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs	Reduction of survivin gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Antitumor assay	5 mg/kg	2 weeks	Antitumor activity against human MDA-MB-231 cells expressing active Stat3 xenografted in mouse at 5 mg/kg, iv for every 3 days for 2 weeks	17463090
NIH3T3	Growth inhibition assay	100 uM		Growth inhibition of mouse NIH3T3 cells expressing v-Ras at 100 uM for every 3 days by soft-agar colony-formation assay	17463090
NIH3T3	Growth inhibition assay	100 uM		Growth inhibition of mouse NIH3T3 cells expressing v-Src at 100 uM for every 3 days by soft-agar colony-formation assay	17463090
MDA-MB-231	Growth Inhibition Assay		72 h	IC50＞100 μM	20072652
SK-BR-3	Growth Inhibition Assay		72 h	IC50＞100 μM	20072652
PANC-1	Growth Inhibition Assay		72 h	IC50＞100 μM	20072652
HPAC	Growth Inhibition Assay		72 h	IC50＞100 μM	20072652
U373	Growth Inhibition Assay		72 h	IC50=52.5 μM	20072652
U87	Growth Inhibition Assay		72 h	IC50=55.1 μM	20072652
T-cell	Growth Inhibition Assay			IC50=50 μM	24068731
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

NSC 74859 (S3I-201)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(In Vitro)
体外研究活性	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]
激酶实验	体外Stat3 DNA结合实验和EMSA分析
激酶实验	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	细胞系	HCC细胞系包括HepG2, PLC/PRF/5, SNU-449, Huh-7, SNU-398, SNU-182，和SNU-475
	浓度	25到250 μM
	孵育时间	72小时
	方法	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。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	STAT3 / p-STAT3 / Cyclin D1 / Bcl-2 / Nanog / OCT4 / ALDH1 / CD44 PD-L1		26556875
	Immunofluorescence	p-STAT3 Oct4 / Twist		26556875
	Growth inhibition assay	Cell viability		26813676

体内研究(In Vivo)
体内研究活性	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]
动物实验	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。

参考文献
[1] Siddiquee K, et al. Proc Natl Acad Sci U S A, 2007, 104(18), 7391-7396. [2] Lin L, et al. Oncogene, 2009, 28(7), 961-972. [3] Chen W, et al. Liver Int, 2012, 32(1), 70-77. [4] Sen N, et al. Proc Natl Acad Sci U S A, 2012, 109(2), 600-605. + 展开

参考文献

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

+ 展开

化学信息&溶解度

分子量	365.36	分子式	C₁₆H₁₅NO₇S
CAS号	501919-59-1	SDF	Download NSC 74859 (S3I-201) SDF
Smiles	CC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 73 mg/mL ( (199.8 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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 μL 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

%DMSO+ %

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。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，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。

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。

* 必填项

* 姓名 请输入您的姓名

* 邮箱 请输入您的邮箱地址 请输入一个有效的邮箱地址

电话

* 留言内容 请写点东西给我们

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):