Stattic

製品コードS7024 バッチS702407

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₈H₅NO₄S

分子量

211.19

CAS No.

19983-44-9

Solubility (25°C)*

体外

DMSO

125 mg/mL (591.88 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (4.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.9 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.800mg/ml (3.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.
in vitro	Stattic inhibits binding of a phosphotyrosine-containing peptide derived from the gp130 receptor to the STAT3 SH2 domain in a strongly temperature-dependent manner. This compound only has a very weak effect on binding of a tyrosinephosphorylated peptide to the SH2-domain of the tyrosine kinase Lck. And it doesn’t inhibit dimerization of two other dimeric transcription factors (c-Myc/Max and Jun/Jun). It also inhibits fluorescein-labeled phosphopeptides to the SH2 domains of STAT1 and STAT5b. This chemical selectively inhibits DNA binding of STAT3 homodimers at a concentration of 10 μM. Shown to inhibit cellular phosphorylation of STAT3 at Tyr705 with little effect towards STAT1 phosphorylation at Tyr701 (in HepG2 cells) or the phosphorylation of JAK1, JAK2, and c-Src (in MDA-MB-231 and MDA-MB-235S cells). This compound increases the apoptotic rate of STAT3-dependent breast cancer cell lines. ^[1]
特徴	Stattic is the first non-peptide small molecule with inhibitory activity against STAT3 SH2 domain regardless of the STAT3 phosphorylation state in vitro.

プロトコル(参考用のみ)

キナーゼアッセイ	High-Throughput Screening and FluorescencePolarization Assays
キナーゼアッセイ	Screening is performed at approximately 30 °C. The specificity of screening hits is validated in analogous assays for binding of the test compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays is 10 mM HEPES (pH 7.5), 1 mM EDTA, 0.1% Nonidet P-40, 50 mM NaCl, and 10% DMSO. The absence of dithiothreitol is essential for inhibitory activity. The sequences of the peptides are: STAT3, 5-carboxyfluorescein-GY(PO₃H₂)LPQTV-NH₂; STAT1, 5-carboxyfluorescein-GY(PO₃H₂)DKPHVL; STAT5, 5-carboxyfluorescein-GY(PO₃H₂)LVLDKW; and Lck, 5-carboxyfluorescein-GY(PO₃H₂)EEIP. For specificity analysis at 30 °C, proteins are used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins are used at 370 nM (STAT3) or 100 nM (Lck). Proteins are incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Before measurement at room temperature, the mixtures are allowed to equilibrate for at least 30 min. Test compounds are used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves are fitted with SigmaPlot. All competition curves are repeated three times in independent experiment
細胞アッセイ	細胞株	Ly3 cells
	濃度	~2.5 μM
	反応時間	48 h
	実験の流れ	MTS
動物実験	動物モデル	Ly3 parental NOD/SCID IL2R null xenograft
	投薬量	3.75 mg/kg every day
	投与方法	intra tumor

参考

https://pubmed.ncbi.nlm.nih.gov/17114005/
https://pubmed.ncbi.nlm.nih.gov/21521803/

カスタマーフィードバック

: Data from [Data independently produced by FEBS Lett, 2014, 10.1016/j.febslet.2014.11.023]

: Data from [J Biol Chem, 2013, 288(8), 5553-61]

: , , Sci Rep, 2017, 7:41404

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：

LSD1 inhibition attenuates targeted therapy-induced lineage plasticity in BRAF mutant colorectal cancer [ Mol Cancer, 2025, 24(1):122]	PubMed: 40264166
Renal tubular GSDME protects cisplatin nephrotoxicity by impeding OGT-STAT3-S100A7A axis in male mice [ Nat Commun, 2025, 16(1):6807]	PubMed: 40707439
Constitutive expression of the transcriptional co-activator IκBζ promotes melanoma growth and immunotherapy resistance [ Nat Commun, 2025, 16(1):5387]	PubMed: 40562773
Gut microbial metabolite 4-hydroxybenzeneacetic acid drives colorectal cancer progression via accumulation of immunosuppressive PMN-MDSCs [ J Clin Invest, 2025, 135(11)e181243]	PubMed: 40179015
Parabacteroides distasonis promotes liver regeneration by increasing β-hydroxybutyric acid (BHB) production and BHB-driven STAT3 signals [ Acta Pharm Sin B, 2025, 15(3):1430-1446]	PubMed: 40370533
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
VSIG4+ tumor-associated macrophages mediate neutrophil infiltration and impair antigen-specific immunity in aggressive cancers through epigenetic regulation of SPP1 [ J Exp Clin Cancer Res, 2025, 44(1):45]	PubMed: 39920772
Lactobacillus johnsonii-derived extracellular vesicles carrying GAPDH protect against ulcerative colitis through modulating macrophage polarization [ J Adv Res, 2025, S2090-1232(25)00444-8]	PubMed: 40533059
Triptolide alleviates acute lung injury by reducing mitochondrial dysfunction mediated ferroptosis through the STAT3/p53 pathway [ Free Radic Biol Med, 2025, 230:79-94]	PubMed: 39914683
Methylstat sensitizes ovarian cancer cells to PARP-inhibition by targeting the histone demethylases JMJD1B/C [ Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z]	PubMed: 39915607

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。