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S3I-201

产品编号 T2505 CAS 501919-59-1

别名: S3I 201, S3I201

S3I-201 (S3I-201) 是一种选择性Stat3抑制剂，IC50为 86 μM。

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S3I-201, CAS 501919-59-1

规格	价格/CNY	货期
5 mg	￥ 415	现货
10 mg	￥ 583	现货
50 mg	￥ 1,465	现货
100 mg	￥ 2,734	现货
200 mg	￥ 3,554	现货
1 mL * 10 mM (in DMSO)	￥ 441	现货

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选择批次

纯度: 99.05%

纯度: 96.05%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	S3I-201 (S3I-201) is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1/5.
靶点活性	STAT3:86 nM (cell free)
体外活性	S3I-201 inhibits Stat3.Stat3 complex formation and Stat3 DNA-binding and transcriptional activities. Furthermore, S3I-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3. Constitutively dimerized and active Stat3C and Stat3 SH2 domain rescue tumor cells from S3I-201-induced apoptosis [1]. Preincubation of CD4 T cells from p53(null)CD45.1 mice with various concentrations of S31-201 suppressed IL-6-induced phosphorylation of STAT3 in a dose-dependent manner as early as 15 min after IL-6 addition. Based on the level of suppression of STAT3 phosphorylation, the IC50 of this inhibitor was determined as 38 μM [2]. Although none of these cell lines was sensitive to S3I-201 (S3I-201) alone, S3I-201 potentiated the antiproliferative effect of cetuximab in all three cell lines (HepG2, SK-HEP1, and Huh-7 cells) [3].
体内活性	Compared with control tumors, which continued to grow, human breast tumors in mice that received S3I-201 displayed strong growth inhibition. Strong inhibition of Stat3 DNA-binding activity in residual tumor tissue from mice treated with S3I-201 compared with control tumor [1]. 8- to 10-wk-old p53nullCD45.1 mice were treated with S31-201 3×/wk at 5 mg/kg, using PBS-treated age-matched p53nullCD45.1 mice as controls. STAT3 phosphorylation in the spleen of S31-201-treated mice was markedly reduced as compared with those treated with PBS [2]. S3I-201 attenuated somatotroph tumor growth and GH secretion in a rat xenograft model [4].
激酶实验	Briefly, 100 ml of biotinyl-e-Ac-EPQpYEEIEL-OH (in 50 mM Tris/150 mM NaCl, pH 7.5) was added to each well of streptavidin-coated 96-well microtiter plates and incubated with shaking at 4°C overnight. Then plates were rinsed with PBS/Tween 20 and then two times with 200 ml of BSA-T-PBS (0.2% BSA/0.1% Tween 20/PBS). Then 50 ml of Lck-SH2-GST fusion protein (6.4 ng/ml in BSA-T-PBS) was added to each well of the 96-well plate in the presence and absence of 50 ml of S3I-201 (for 30 and 100 mM final concentrations), and the plate was shaken at room temperature for 4 h. After solutions were removed, each well was rinsed four times with BSA-T-PBS (200 ml), and 100 ml of polyclonal rabbit anti-GST antibody (100 ng/ml in BSA-T-PBS) was added to each well and incubated at 4°C overnight. After washing with BSA-T-PBS, 100 ml of 200 ng/ml BSA-T-PBS horseradish peroxidase-conjugated mouse anti-rabbit antibody was added to each well and incubated for 45 min at room temperature. After four washing steps with BSA-T-PBS and three washing steps with PBS-T, 100 ml of peroxidase substrate was added to each well and incubated for 5-15 min. The peroxidase reaction was stopped by adding 100 ml of 1 M sulfuric acid solution, and absorbance was read at 450 nm with an ELISA plate reader [1].
细胞实验	Proliferating cells were treated with or without S3I-201 for up to 48 h. In some cases, cells were first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24–48 h. Cells were then detached and analyzed by annexin V binding according to the manufacturer's protocol and flow cytometry to quantify the percent apoptosis [1].
动物实验	Six-week-old female athymic nude mice were purchased from Harlan and maintained in the institutional animal facilities approved by the American Association for Accreditation of Laboratory Animal Care. Athymic nude mice were injected in the left flank area s.c. with 5 × 10^6 human breast cancer MDA-MB-231 cells in 100 μl of PBS. After 5–10 days, tumors with a diameter of 3 mm were established. Animals were given S3I-201 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals were stratified so that the mean tumor sizes in all treatment were nearly identical. Tumor volume was calculated according to the formula V = 0.52 × a2× b, where a is the smallest superficial diameter and b is the largest superficial diameter [1].

别名	S3I 201, S3I201
分子量	365.36
分子式	C16H15NO7S
CAS No.	501919-59-1

存储

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

溶解度

DMSO: 36.5 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.737 mL	13.6851 mL	27.3703 mL	68.4257 mL
	5 mM	0.5474 mL	2.737 mL	5.4741 mL	13.6851 mL
	10 mM	0.2737 mL	1.3685 mL	2.737 mL	6.8426 mL
	20 mM	0.1369 mL	0.6843 mL	1.3685 mL	3.4213 mL
	50 mM	0.0547 mL	0.2737 mL	0.5474 mL	1.3685 mL
	100 mM	0.0274 mL	0.1369 mL	0.2737 mL	0.6843 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Siddiquee K, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. 2. Zhang S, et al. Trp53 negatively regulates autoimmunity via the STAT3-Th17 axis. FASEB J. 2011 Jul;25(7):2387-98. 3. Chen W, et al. NSC 74859-mediated inhibition of STAT3 enhances the anti-proliferative activity of cetuximab in hepatocellular carcinoma. Liver Int. 2012 Jan;32(1):70-7. 4. Zhou C, et al. STAT3 upregulation in pituitary somatotroph adenomas induces growth hormone hypersecretion. J Clin Invest. 2015 Apr;125(4):1692-702 5. Chen X J, He M J, Zhou G. All‐trans retinoic acid induces anti‐tumor effects via STAT 3 signaling inhibition in oral squamous cell carcinoma and oral dysplasia[J]. Journal of Oral Pathology & Medicine. 2019.

文献引用

1. Xue J, Liao Q, Luo M, et al. Cigarette smoke-induced oxidative stress activates NRF2 to mediate fibronectin disorganization in vascular formation. Open Biology. 2022, 12(4): 210310 2. Chen X J, He M J, Zhou G. All‐trans retinoic acid induces anti‐tumor effects via STAT 3 signaling inhibition in oral squamous cell carcinoma and oral dysplasia. Journal of Oral Pathology & Medicine.. 2019

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

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

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

S3I-201 501919-59-1 JAK/STAT signaling Stem Cells STAT Inhibitor S3I 201 inhibit NSC74859 NSC 74859 S3I201 NSC-74859 inhibitor

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S3I-201

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords