NSC 74859 (S3I-201)

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

NSC 74859 (S3I-201) Chemical Structure

CAS: 501919-59-1

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
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客户使用Selleck的NSC 74859 (S3I-201)发表文献218

产品质控

批次: 纯度: 99.28%
98.91

NSC 74859 (S3I-201)相关产品

相关信号通路图

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
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4oC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),4oC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。

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)

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

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)

mg/kg g μL

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,: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: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: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。

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