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Stattic

Stattic

产品编号 T6308   CAS 19983-44-9
别名: STAT3 Inhibitor V

Stattic (STAT3 Inhibitor V) 是一种 STAT3 抑制剂 (IC50=5.1 μM),选择性地抑制 STAT3 活化、二聚化和核转位。Stattic 具有抗肿瘤活性,可诱导细胞凋亡

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Stattic Chemical Structure
Stattic, CAS 19983-44-9
规格 价格/CNY 货期 数量
5 mg ¥ 257 现货
10 mg ¥ 389 现货
25 mg ¥ 663 现货
50 mg ¥ 997 现货
100 mg ¥ 1,660 现货
200 mg ¥ 2,470 现货
500 mg ¥ 3,970 现货
1 mL * 10 mM (in DMSO) ¥ 389 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Stattic (T6308)
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选择批次  
纯度: 99.76%
纯度: 99.64%
纯度: 98.78%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
靶点活性 STAT3:5.1 μM (cell free)
体外活性 方法:人胰腺癌细胞 PANC-1 和 BxPc-3 用 Stattic (1-10 μM) 处理 12-48 h,使用 CCK-8 方法检测细胞活力。
结果:Stattic 以浓度和时间依赖的方式降低 PANC-1 和 BxPc-3 细胞增殖。Stattic 处理 24 h 后对 BxPc-3 和 PANC-1 细胞的 IC50 分别为 3.135-5.296 μM 和 3.835-4.165 μM。[1]
方法:人肝癌细胞 HepG2 用 Stattic (5-20 μM) 处理 1 h,随后用 IL-6 或 IFN-γ刺激,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Stattic 的预孵育导致 STAT3 Tyr705 的磷酸化选择性降低,而 STAT1 Tyr701 的激活保持不变。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Stattic (10 mg/kg) 腹腔注射给携带人胰腺癌肿瘤 PANC-1 的 BALB/c nude 小鼠,每天一次,持续四周。
结果:Stattic 通过灭活 STAT3 来抑制裸鼠肿瘤模型中的 PC 生长。[1]
方法:为研究在急性肝损伤中的作用,将 Stattic (5 mg/kg in DMSO:olive oil = 1:19) 单次腹腔注射给  LPS/d-GalN 诱导急性肝损伤的 BALB/c 小鼠。
结果:Stattic 对 LPS/d-GalN 诱导的肝损伤具有保护作用,其保护作用可能与其抗炎和抗凋亡作用有关。[3]
激酶实验 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].
细胞实验 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].
别名 STAT3 Inhibitor V
分子量 211.19
分子式 C8H5NO4S
CAS No. 19983-44-9

存储

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

溶解度

Ethanol: 1.1 mg/mL (5 mM)

DMSO: 10.6 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 4.7351 mL 23.6754 mL 47.3507 mL 118.3768 mL
5 mM 0.947 mL 4.7351 mL 9.4701 mL 23.6754 mL
DMSO 10 mM 0.4735 mL 2.3675 mL 4.7351 mL 11.8377 mL
20 mM 0.2368 mL 1.1838 mL 2.3675 mL 5.9188 mL
50 mM 0.0947 mL 0.4735 mL 0.947 mL 2.3675 mL

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TargetMol Library Books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.

TargetMol Library Books文献引用

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.
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GSK2795039 Bortezomib Domatinostat Sorafenib tosylate Etidronic acid SRT 2183 STAT3-IN-1 Doxorubicin hydrochloride

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 经典已知活性库 抗前列腺癌化合物库 抗衰老化合物库 抗癌细胞代谢库 抗肺癌化合物库 癌细胞分化化合物库 抗胰腺癌化合物库 NO PAINS 化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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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

 

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