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- CAS号：
19983-44-9
- 规格：
1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥327.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥221.0 |
| 规格： | 10mg | 产品价格： | ￥327.0 |
| 规格： | 25mg | 产品价格： | ￥530.0 |
| 规格： | 50mg | 产品价格： | ￥797.0 |
| 规格： | 100mg | 产品价格： | ￥1328.0 |
| 规格： | 200mg | 产品价格： | ￥1976.0 |
| 规格： | 500mg | 产品价格： | ￥3176.0 |
Product Introduction
Bioactivity
| 名称 | Stattic |
| 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. |
| 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]. |
| 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]. |
| 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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 1.1 mg/mL (5.21 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.06 mg/mL (5.02 mM), Solution. DMSO : 260 mg/mL (1231.12 mM), Sonication is recommended. |
| 关键字 | Y705 | syndrome | Stattic | STAT3 | STAT | SH2 | S727 | S phase | p-STAT3 | prostate | P-ERK1/2 | PC3M-1E8 | Inhibitor | inhibit | cancer | Apoptosis | Alport |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Immuno-Oncology Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Cancer Metabolism Compound Library | Anti-Diabetic Compound Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | Cancer Cell Differentiation Compound Library | NO PAINS Compound Library | Anti-Lung Cancer Compound Library | Immunology/Inflammation Compound Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 Stattic【19983-44-9】
￥221 - 3176
