Stattic

カタログ番号 T6308 CAS 19983-44-9

別名: STAT3 Inhibitor V

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

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Stattic, CAS 19983-44-9

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 7,000
10 mg	在庫あり	￥ 11,000
25 mg	在庫あり	￥ 18,000
50 mg	在庫あり	￥ 29,000
100 mg	在庫あり	￥ 45,500
200 mg	在庫あり	￥ 67,500
500 mg	在庫あり	￥ 112,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 11,500

バルクのお問い合わせ

バッチを選択

純度: 99.76%

COA DATASHEET SDS HNMR HPLC

純度: 99.64%

COA DATASHEET SDS HPLC HNMR

純度: 98.78%

COA DATASHEET SDS HPLC HNMR

COA DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.
ターゲット＆IC50	STAT3:5.1 μM (cell free)
In vitro	METHODS: Human pancreatic cancer cells PANC-1 and BxPc-3 were treated with Stattic (1-10 μM) for 12-48 h. Cell viability was measured using the CCK-8. RESULTS: Stattic decreased the proliferation of PANC-1 and BxPc-3 cells in a concentration- and time-dependent manner, and the IC50s of Stattic on BxPc-3 and PANC-1 cells were 3.135-5.296 μM and 3.835-4.165 μM, respectively, after treatment with Stattic for 24 h. [1] METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Stattic (5-20 μM) for 1 h, followed by stimulation with IL-6 or IFN-γ, and the expression levels of target proteins were detected by Western Blot. RESULTS: Pre-incubation with Stattic resulted in a selective decrease in the phosphorylation of STAT3 Tyr705, while the activation of STAT1 Tyr701 remained unchanged. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Stattic (10 mg/kg) was administered intraperitoneally once daily for four weeks to BALB/c nude mice harboring human pancreatic adenocarcinoma tumor PANC-1. RESULTS: Stattic inhibited PC growth in a nude mouse tumor model by inactivating STAT3. [1] METHODS: To investigate the role in acute liver injury, Stattic (5 mg/kg in DMSO:olive oil = 1:19) was administered as a single intraperitoneal injection to BALB/c mice with LPS/d-GalN induced acute liver injury. RESULTS: Stattic was protective against LPS/d-GalN-induced liver injury, and its protective effect may be related to its anti-inflammatory and anti-apoptotic effects. [3]
キナーゼ試験	The screening was performed at approximately 30C. The specificity of screening hits was 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 was 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 were: 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. Peptides were >95% pure. For specificity analysis at 30°C, proteins were used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37°C, proteins were used at 370 nM (STAT3) or 100 nM (Lck). Proteins were incubated with test compounds in tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Analysis of c-Myc/Max and Jun/Jun dimerization and DNA binding at 37°C was performed as described but in the absence of DTT. Before measurement at room temperature, the mixtures were allowed to equilibrate for at least 30 min. Test compounds were used at the indicated concentrations diluted from 20× stock in DMSO. Binding curves and inhibition curves were fitted with SigmaPlot. All competition curves were repeated three times in independent experiments. For the analysis of time dependence of the inhibition, the components were mixed from stock solutions kept at 0C and then incubated at 37C. Aliquots were taken at the indicated time points [1].
細胞研究	MDA-MB-231, MDA-MB-435S, and MDA-MB-453 cells were seeded. at 5 × 10^4 cells in 6-well plates, grown for 24 hr before adding DMSO or Stattic (final DMSO concentration 0.1%) and then incubated with the inhibitor for 24 hr. All cells were collected and resuspended in buffer (0.1% sodium citrate, 0.1% Triton X-100, 20 μM propidium iodide) and incubated for 3 hr before 10^4 cells per sample were analyzed by flow cytometry with a FACSCalibur equipped with a 488 nm laser [1].

別名	STAT3 Inhibitor V
分子量	211.19
分子式	C8H5NO4S
CAS No.	19983-44-9

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: 1.1 mg/mL (5 mM)

DMSO: 55 mg/mL (260.43 mM)

参考文献

1. Guo H, et al. Inhibition of STAT3Y705 phosphorylation by Stattic suppresses proliferation and induces mitochondrial-dependent apoptosis in pancreatic cancer cells. Cell Death Discov. 2022 Mar 14;8(1):116. 2. Schust J, et al. Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. Chem Biol. 2006 Nov;13(11):1235-42. 3. Li S, et al. Stattic alleviates acute hepatic damage induced by LPS/d-galactosamine in mice. Innate Immun. 2021 Feb;27(2):201-209. 4. Zhao C, Zhang B, Jiang J, et al. Up-regulation of ANXA1 suppresses polymorphonuclear neutrophil infiltration and myeloperoxidase activity by activating STAT3 signaling pathway in rat models of myocardial ischemia-reperfusion injury[J]. Cellular signalling. 2019, 62: 109325. 5. Lin I Y, Pan M H, Lai C S, et al. CCM111, the water extract of Antrodia cinnamomea, regulates immune-related activity through STAT3 and NF-κB pathways[J]. Scientific Reports. 2017 Jul 7;7(1):4862. 6. Ning T, Guo J, Zhang K, et al. Nanosecond pulsed electric fields enhanced chondrogenic potential of mesenchymal stem cells via JNK/CREB-STAT3 signaling pathway[J]. Stem cell research & therapy. 2019 Jan 24;10(1):45. 7. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells[J]. Frontiers in immunology. 2020, 11.

引用文献

1. Wang X, Li X, Wang J, et al. SMGL-1/NBAS acts as a RAB-8 GEF to regulate unconventional protein secretion. Journal of Cell Biology. 2022, 221(7): e202111125 2. Li K, Fan L, Lin J, et al. Nanosecond pulsed electric fields prime mesenchymal stem cells to peptide ghrelin and enhance chondrogenesis and osteochondral defect repair in vivo. Science China Life Sciences. 2021: 1-13. 3. Zhang T, Wang Y, Li Q, et al. Mesenchymal stromal cells equipped by IFNα empower T cells with potent anti-tumor immunity. Oncogene. 2022: 1-16. 4. Zheng Q W, Ni Q Z, Zhu B, et al. PPDPF promotes lung adenocarcinoma progression via inhibiting apoptosis and NK cell-mediated cytotoxicity through STAT3. Oncogene. 2022: 1-13. 5. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells. Frontiers in immunology. 2021 Jan 29;11:615868. doi: 10.3389/fimmu.2020.615868. eCollection 2020. 6. Ning T, Guo J, Zhang K, et al. Nanosecond pulsed electric fields enhanced chondrogenic potential of mesenchymal stem cells via JNK/CREB-STAT3 signaling pathway. Stem Cell Research & Therapy. 2019 Jan 24;10(1):45 7. Lin I Y, Pan M H, Lai C S, et al. CCM111, the water extract of Antrodia cinnamomea, regulates immune-related activity through STAT3 and NF-κB pathways. Scientific Reports. 2017, 7(1): 1-13 8. Zheng J M, Zhou H X, Yu H Y, et al. By Increasing the Expression and Activation of STAT3, Sustained C5a Stimulation Increases the Proliferation, Migration, and Invasion of RCC Cells and Promotes the Growth of Transgrafted Tumors. Cancer Management and Research. 2021, 13: 7607-7621. 9. Zhao C, Zhang B, Jiang J, et al. Up-regulation of ANXA1 suppresses polymorphonuclear neutrophil infiltration and myeloperoxidase activity by activating STAT3 signaling pathway in rat models of myocardial ischemia-reperfusion injury. Cellular Signalling. 2019, 62: 109325 10. He S, Lu M, Zhang L, et al.RSK4 promotes the macrophage recruitment and M2 polarization in esophageal squamous cell carcinoma.Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease.2023: 166996.

11. Yu L, Xu L, Chen Y, et al.IDO1 Inhibition Promotes Activation of Tumor-intrinsic STAT3 Pathway and Induces Adverse Tumor-protective Effects.The Journal of Immunology.2024 12. Liu H, Sun L, Zhao H, et al.Proteinase 3 depletion attenuates leukemia by promoting myeloid differentiation.Cell Death & Differentiation.2024: 1-14.

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Stattic 19983-44-9 Apoptosis JAK/STAT signaling Stem Cells STAT inhibit Alport PC3M-1E8 cancer p-STAT3 prostate S727 syndrome Inhibitor P-ERK1/2 SH2 STAT3 Inhibitor V S phase Y705 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Stattic

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords