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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STAT1和STAT5的抑制活性低。
NSC 74859 (S3I-201) Chemical Structure
CAS: 501919-59-1
產(chǎn)品質(zhì)控
批次：
純度：
99.28%
99.28
NSC 74859 (S3I-201)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | STAT1 STAT3 STAT5 STAT6 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Stattic Cryptotanshinone (Tanshinone C) SH-4-54 C188-9 (TTI-101) BP-1-102 Napabucasin (BBI608) HO-3867 Nifuroxazide AS1517499 Homoharringtonine (HHT) STAT5-IN-1 Ochromycinone (STA-21) HJC0152 APTSTAT3-9R STAT3-IN-1 SC-1 SH5-07 (SH-5-07) Scutellarin Narciclasine | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 酪氨酸激酶抑制劑分子庫 JAK-STAT信號通路庫 | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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STAT1和STAT5的抑制活性低。 | ||
|---|---|---|---|
| 特性 | S3I-201是化學(xué)探測器抑制劑，可以除去乳腺瘤。 | ||
| 靶點(diǎn) |
|
| 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] |
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|---|---|---|---|---|
| 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。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 | |||
| 孵育時間 | 72小時 | |||
| 方法 | 5 ×103個細(xì)胞接種在含完全培養(yǎng)基的96孔微型板上。培養(yǎng)72小時后，每孔加入100 μL 2 mg/mL MTT溶液測量存活細(xì)胞數(shù)。2小時后，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。 |
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| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(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作用于攜帶人類乳腺癌(MDA-MB-231)的鼠時，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，沒有明顯的外部健康改變或者體重減輕癥狀。[2] |
|
|---|---|---|
| 動物實(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 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 73 mg/mL ( (199.8 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(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：如該濃度超過該批次藥物DMSO溶解度，請先聯(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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