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
CAS: 501919-59-1
产品质控
批次：
纯度：
99.28%
99.28
NSC 74859 (S3I-201)相关产品
相关信号通路图
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 |
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| 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 抗增殖效果。[3] |
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|---|---|---|---|---|
| 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。 |
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| 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 |
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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] |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解配方 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
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
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。
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