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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C8H5NO4S |
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| 分子量 | 211.19 | CAS No. | 19983-44-9 | |
| Solubility (25°C)* | 体外 | DMSO | 42 mg/mL (198.87 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | 初の非ペプチド小分子であるStatticは、無細胞アッセイにおいて5.1 μMのIC50でSTAT3活性化と核内移行を強力に阻害し、STAT1に対して高い選択性を示します。Statticはアポトーシスを誘発します。 |
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| 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. |
| 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 | |
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| 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 |
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| 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
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カスタマーフィードバック
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Data from [Data independently produced by FEBS Lett, 2014, 10.1016/j.febslet.2014.11.023]
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Data from [J Biol Chem, 2013, 288(8), 5553-61]
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, , Sci Rep, 2017, 7:41404
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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。