NSC 74859 (S3I-201)

製品コードS1155 バッチS115502

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H15NO7S
分子量 365.36 CAS No. 501919-59-1
Solubility (25°C)* 体外 DMSO 73 mg/mL (199.8 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro

NSC 74859 (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 activities. Moreover, it also inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin. [1] This compound 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 it potentiates the antiproliferative effect in HepG2 and Huh-7 cells via the STAT3 signalling pathway. [3]
in vivo

NSC 74859 (S3I-201) shows the antitumor efficacy in mouse models with human breast tumor xenografts that harbor constitutively active Stat3 at a dose of 5 mg/kg (i.v. every 2 or every 3 days). [1] This compound 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]
特徴 A chemical probe inhibitor of Stat3 activity.

プロトコル(参考用のみ)

キナーゼアッセイ 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 NSC 74859 (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
細胞アッセイ 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 NSC 74859 (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.
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.
投薬量 ≤5 mg/kg
投与方法 Administered via i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17463090/
  • https://pubmed.ncbi.nlm.nih.gov/19137011/
  • https://pubmed.ncbi.nlm.nih.gov/22098470/
  • https://pubmed.ncbi.nlm.nih.gov/22190485/

カスタマーフィードバック

Data from [Data independently produced by Mol Cancer, 2014, 13:176]

Data from [Data independently produced by Int Immunopharmacol, 2014, 20(1), 117-23]

Data from [Data independently produced by Microbes Infect, 2014, 16(1), 17-27]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cancer-associated fibroblast derived CXCL14 drives cisplatin chemoresistance by enhancing nucleotide excision repair in bladder cancer [ J Exp Clin Cancer Res, 2025, 44(1):265] PubMed: 40898244
Natural small molecule bergapten ameliorates rheumatoid arthritis by targeting STAT3 [ Pharmacol Res, 2025, 219:107878] PubMed: 40714303
Polarization of Vδ2 T cells to a Th2-like phenotype promotes plasmablast differentiation and possesses pro-fibrotic properties in IgG4-related disease [ Front Immunol, 2025, 16:1550405] PubMed: 40213561
SYT7 accelerates nasopharyngeal carcinoma progression via ALDH1A3-mediated STAT3 signaling activation [ Oncogenesis, 2025, 14(1):16] PubMed: 40346036
KLHL25-ACLY module functions as a switch in the fate determination of the differentiation of iTreg/Th17 [ Commun Biol, 2025, 8(1):471] PubMed: 40119138
Intrapleural dual blockade of IL-6 and PD-L1 reprograms CAF dynamics and the tumor microenvironment in lung cancer-associated malignant pleural effusion [ Respir Res, 2025, 26(1):180] PubMed: 40349069
Suberosin attenuates rheumatoid arthritis by repolarizing macrophages and inhibiting synovitis via the JAK/STAT signaling pathway [ Arthritis Res Ther, 2025, 27(1):12] PubMed: 39838477
Regulation of keratinocyte barrier function and inflammatory response by the EGFR-STAT3 Pathway: Potential therapeutic implications of osimertinib and afatinib [ Cytokine, 2025, 185:156802] PubMed: 39612655
Effect of Anti-S100A4 Monoclonal Antibody Treatment on Experimental Skin Fibrosis and Systemic Sclerosis-Specific Transcriptional Signatures in Human Skin [ Arthritis Rheumatol, 2024, 76(5):783-795] PubMed: 38108109
Augmented ERO1α upon mTORC1 activation induces ferroptosis resistance and tumor progression via upregulation of SLC7A11 [ J Exp Clin Cancer Res, 2024, 43(1):112] PubMed: 38610018

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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