NSC 74859 (S3I-201)

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.

NSC 74859 (S3I-201)化学構造

CAS No. 501919-59-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 14900 国内在庫あり
JPY 13600 国内在庫あり
JPY 21900 国内在庫あり
JPY 63400 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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NSC 74859 (S3I-201)関連製品

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 of cetuximab in HepG2 and Huh-7 cells via the STAT3 signalling pathway. [3]
Kinase Assay In vitro Stat3 DNA-binding assay and EMSA analysis
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, and the formazan crystals are dissolved by adding 100 μL dimethylsulfoxide per well. 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.

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

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

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)

mg/kg g μL

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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