NSC 74859 (S3I-201)

製品コード：S1155 純度：99.28%

NSC 74859 (S3I-201) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.

CAS No. 501919-59-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 34000	国内在庫あり
50mg	JPY 85500	国内在庫あり
1g	JPY 405000	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（229）

製品安全説明書

現在のバッチを見る：純度： 99.28%

99.28

NSC 74859 (S3I-201)関連製品

関連ターゲット	STAT1 STAT3 STAT5 STAT6	もっと見る
関連製品	Stattic Cryptotanshinone (Tanshinone C) SH-4-54 C188-9 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 Narciclasine SH5-07 (SH-5-07) Scutellarin	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	もっと見る

シグナル伝達経路

STATシグナル伝達経路

STAT阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	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
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生物活性

製品説明

NSC 74859 (S3I-201) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.

特性

A chemical probe inhibitor of Stat3 activity.

Targets

STAT3 ^[1]
(Cell-free assay)

86 μM

In Vitro
In vitro	S3I-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3 by inhibiting Stat3·Stat3 complex formation and Stat3 DNA-binding and transcriptional activitie. Moreover, S3I-201 also inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin. ^[1] S3I-201 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with IC50 of 100 μM. In addition, the cells with impaired TGF-β signaling are four times as sensitive to the STAT3 inhibitor S3I-201. ^[2] A recent study shows that S3I-201 potentiates the antiproliferative effect in HepG2 and Huh-7 cells via the STAT3 signalling pathway. ^[3]
Kinase Assay	In vitro Stat3 DNA-binding assay and EMSA analysis
Kinase Assay	Briefly, 100 mL of biotinyl-e-Ac-EPQpYEEIEL-OH (in 50 mM Tris/150 mM NaCl, pH 7.5) is added to each well of streptavidin-coated 96-well microtiter plates and incubated with shaking at 4 °C overnight. Then plates are rinsed with PBS/Tween 20 and then two times with 200 mL of BSA-T-PBS (0.2% BSA/0.1% Tween 20/PBS). Then 50 mL of Lck-SH2-GST fusion protein (6.4 ng/ml in BSA-T-PBS) is added to each well of the 96-well plate in the presence and absence of 50 mL of S3I-201 (for 30 and 100 mM final concentrations), and the plate is shaken at room temperature for 4 hours. After solutions are removed, each well is rinsed four times with BSA-T-PBS (200 mL), and 100 mL of polyclonal rabbit anti-GST antibody (100 ng/mL in BSA-T-PBS) is added to each well and incubated at 4 °C overnight. After washing with BSA-T-PBS, 100 mL of 200 ng/mL BSA-T-PBS horseradish peroxidase-conjugated mouse anti-rabbit antibody is added to each well and incubated for 45 minutes at room temperature. After four washing steps with BSA-T-PBS and three washing steps with PBS-T, 100 mL of peroxidase substrate is added to each well and incubated for 5-15 minutes. The peroxidase reaction is stopped by adding 100 mL of 1 M sulfuric acid solution, and absorbance is read at 450 nm with an ELISA plate rea
細胞実験	細胞株	MDA-MB-435, MDA-MB-453 and MDA-MB-231 cells lines
	濃度	~ 250 μM
	反応時間	72 hours
	実験の流れ	The MTT assay is based on the conversion of the yellow tetrazolium salt MTT to purple formazan crystals by metabolically active cells. The MTT assay provides a quantitative determination of viable cells. Cells are seeded in 96-well microplates in complete culture medium in the absence or presence of increasing serial dosages of S3I-201 as indicated. At 72 hours after culture, the number of viable cells is measured by adding 100 μL/well of 2 mg/mL MTT solution. After 2 hours, the medium is removed. The absorbance is read at 590 nm with an enzyme-linked immunosorbent assay reader. Each treatment point is performed in 10 wells or sextuplicate.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	S3I-201 (5 mg/kg, i.v. every 2 or every 3 days) shows the antitumor efficacy in mouse models with human breast tumor xenografts that harbor constitutively active Stat3. ^[1] S3I-201 treatment reduces Varicella-zoster virus (VZV) replication on the basis of the bioluminescence signal and the number of positive skin xenografts compared with DMSO-treated mice by inhibiting STAT3 phosphorylation. ^[4]
動物実験	動物モデル	Human breast cancer MDA-MB-231 cells are injected s.c. into the left flank of athymic nu/nu mice.
	投与量	≤5 mg/kg
	投与経路	Administered via i.v.

参考
[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. + 展開

参考

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

+ 展開

化学情報

分子量	365.36	化学式	C₁₆H₁₅NO₇S
CAS No.	501919-59-1	SDF	Download NSC 74859 (S3I-201) SDFをダウンロードする
Smiles	CC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (199.8 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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