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NSC 74859 (S3I-201)

NSC 74859 (S3I-201)有效抑制STAT3的DNA結(jié)合活性，IC50為86 μM，而對(duì)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

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 638.93 現(xiàn)貨
5mg 563.02 現(xiàn)貨
10mg 972.36 現(xiàn)貨
50mg 3028.28 現(xiàn)貨
200mg 8165.43 現(xiàn)貨
1g 22113 現(xiàn)貨
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NSC 74859 (S3I-201)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

STAT Signaling Pathways

STAT信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 NSC 74859 (S3I-201)有效抑制STAT3的DNA結(jié)合活性，IC50為86 μM，而對(duì)STAT1和STAT5的抑制活性低。
特性 S3I-201是化學(xué)探測(cè)器抑制劑，可以除去乳腺瘤。
靶點(diǎn)
STAT3 [1]
(Cell-free assay)
86 μM
體外研究(In Vitro)
體外研究活性

S3I-201選擇性抑制Stat3 DNA結(jié)合活性。S3I-201抑制Stat3·Stat3復(fù)合形式,不依賴(lài)于Stat3的激活狀態(tài)。S3I-201不干涉Lck SH2與同源pTyr肽結(jié)合。S3I-201作用于NIH 3T3/v-Src鼠成纖維細(xì)胞和人類(lèi)乳腺癌MDA-MB-231, MDA-MB-435, 和MDA-MB-468 細(xì)胞，可以抑制Stat3激活。S3I-201 抑制Stat3依賴(lài)的轉(zhuǎn)錄活性。 S3I-201 也抑制編碼cyclin D1, Bcl-xL,和surviving 的Stat3-調(diào)節(jié)基因的表達(dá)。[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細(xì)胞。[2]最新研究顯示S3I-201作用于Hep-G2, Huh-7和SK-HEP-1細(xì)胞，加強(qiáng) 抗增殖效果。[3]
激酶實(shí)驗(yàn) 體外Stat3 DNA結(jié)合實(shí)驗(yàn)和EMSA分析
100 mL生物素-e-Ac-EPQpYEEIEL-OH (溶于50 mM Tris/150 mM NaCl, pH 為7.5) 加到鏈霉親和素包被的96孔微型板的每孔中，在4oC下振蕩溫育過(guò)夜。用PBS/Tween-20沖洗板，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，在室溫下振蕩處理4小時(shí)。轉(zhuǎn)移溶液，用200 mL BSA-T-PBS沖洗4次,然后在每孔中加入100 mL多克隆GST抗體 (100 ng/mL，溶于BSA-T-PBS)，4oC下溫育過(guò)夜。用BSA-T-PBS沖洗后, 在每孔中加入100 mL 200 ng/ml BSA-T-PBS辣根過(guò)氧化物酶結(jié)合的二抗，然后在室溫下溫育45分鐘。用BSA-T-PBS沖洗4步后，再用PBS-T沖洗3步，然后在每孔中加入100 mL過(guò)氧化物酶底物，溫育5到15分鐘。加入100 mL 1 M硫酸溶液終止過(guò)氧化物酶反應(yīng)，使用ELISA計(jì)數(shù)板在450nm 處讀取吸光值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 HCC細(xì)胞系包括HepG2, PLC/PRF/5, SNU-449, Huh-7, SNU-398, SNU-182，和SNU-475
濃度 25到250 μM
孵育時(shí)間 72小時(shí)
方法

5 ×103個(gè)細(xì)胞接種在含完全培養(yǎng)基的96孔微型板上。培養(yǎng)72小時(shí)后，每孔加入100 μL 2 mg/mL MTT溶液測(cè)量存活細(xì)胞數(shù)。2小時(shí)后，轉(zhuǎn)移培養(yǎng)基，每孔加入100 μL二甲亞砜溶解甲結(jié)晶。使用酶聯(lián)免疫吸附法計(jì)數(shù)器在590 nm處讀取吸光值。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

5 mg/kg劑量的S3I-201作用于攜帶人類(lèi)乳腺癌(MDA-MB-231)的鼠時(shí)，顯示出強(qiáng)抑制效果。[1]5 mg/kg劑量的S3I-201作用于Huh-7移植瘤，顯示出強(qiáng)抗癌活性，沒(méi)有明顯的外部健康改變或者體重減輕癥狀。[2]
動(dòng)物實(shí)驗(yàn) Animal Models 6周大的攜帶MDA-MB-231移植瘤模型的雌性無(wú)胸腺裸鼠
Dosages 5 mg/kg
Administration 靜脈注射，每周2天或3天。

化學(xué)信息&溶解度

分子量 365.36 分子式

C16H15NO7S
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 73 mg/mL ( (199.8 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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