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NSC 74859

现货
Catalog No.
A8338
Stat3抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 700.00
现货
50mg
¥ 1,760.00
现货
200mg
¥ 5,280.00
现货

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Background

S3I-201 is a selective inhibitor of Stat3 with IC50 value of 86 μM [1].

In the in vitro Stat3 DNA-binding assay, S3I-201 showed potent inhibition of the Stat3 DNA-binding activity with an average IC50 of 86 μM. In the EMSA assay, S3I-201 selectively inhibited Stat3 DNA-binding activity over that of Stat1 and Stat5. It suppressed the complex formation of Stat1-Stat3 and Stat1-Stat1 with IC50 values of 160 and > 300 μM, respectively. Besides that, the unphosphorylated, inactive Stat3 monomer was found to restore the Stat3 DNA-binding activity inhibited by S3I-201, suggesting that the inhibition was independent on the activation status. In NIH 3T3/v-Src fibroblasts, S3I-201 inhibited the constitutive activation of Stat3 and reduced the pTyr-705 Stat3 levels. Moreover, S3I-201 was found to significantly induce apoptosis in cells with constitutively active Stat3 at concentration of 30–100 μM. S3I-201 also reduced the expression of cyclin D1, Bcl-xL and surviving in these cells [1].

References:
[1] Siddiquee K, Zhang S, Guida W C, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proceedings of the National Academy of Sciences, 2007, 104(18): 7391-7396.

文献引用

1. Deng R, Zhang P, et al. "HDAC is indispensable for IFN-γ-induced B7-H1 expression in gastric cancer." Clin Epigenetics. 2018 Dec 11;10(1):153. PMID:30537988
2. Xu J, Li Y, et al. "Baicalin regulates SirT1/STAT3 pathway and restrains excessive hepatic glucose production."Pharmacol Res. 2018 Aug 23;136:62-73. PMID:30144531
3. Yang L, Xu J, et al. "Porcine epidemic diarrhea virus-induced epidermal growth factor receptor activation impairs the antiviral activity of type I interferon." J Virol. 2018 Jan 31. pii: JVI.02095-17. PMID:29386292
4. Zhang ZL, Jiang QC, et al. "Schisandrin A reverses doxorubicin-resistant human breast cancer cell line by the inhibition of P65 and Stat3 phosphorylation." Breast Cancer. 2017 Nov 27. PMID:29181822
5. Marie R.Mooney."Precision Medicine Approaches to Integrating Genomics with Cancer Therapy: Applications in Glioblastoma and Lymphoma." ProQuest LLC..2016

Chemical Properties

StorageStore at -20°C
M.Wt365.36
Cas No.501919-59-1
FormulaC16H15NO7S
SynonymsS3I-201;NSC74859;NSC-74859;S3I 201
Solubility≥18.25mg/mL in DMSO
Chemical Name2-hydroxy-4-[[2-(4-methylphenyl)sulfonyloxyacetyl]amino]benzoic acid
SDFDownload SDF
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

NIH 3T3/v-Src细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

100 μM,24 hours

实验结果

在Flag-Stat3瞬时转染稳定表达Stat3-YFP的病毒Src转化的(NIH 3T3/v-Src)小鼠成纤维细胞中,用NSC-74859处理,然后进行下拉实验和SDS/PAGE。对于全细胞裂解物使用FLAG抗体的Western印迹分析表明,对照和NSC-74859处理的瞬时转染细胞的裂解物中FLAG-ST3蛋白的表达相当。用抗FLAG抗体进行的Western印迹分析显示,NSC-74859处理的细胞的Stat3-YFP免疫沉淀物中没有可检测水平的FLAG-ST3蛋白,表明NSC-74859破坏了Stat3-YFP和FLAG- ST3蛋白形成的复合体。

动物实验: [1]

动物模型

注射MDA-MB-231细胞的雌性无胸腺裸鼠

给药剂量

静脉注射,5 mg/kg,每2或3天一次,持续2周

实验结果

与继续生长的载体处理的对照肿瘤相比,NSC-74859处理的小鼠中,人乳腺肿瘤的生长被强烈抑制。在治疗终止时对治疗小鼠的评价显示肿瘤生长没有恢复,这表明NSC-74859可能对肿瘤生长具有长期持久的作用。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Siddiquee K, Zhang S, Guida W C, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proceedings of the National Academy of Sciences, 2007, 104(18): 7391-7396.

生物活性

Description NSC 74859(S3I-201 )是一种有效的STAT3 DNA结合活性抑制剂,IC50为86 μM。
靶点 Stat3          
IC50 86 μM          

质量控制

化学结构

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859

相关生物数据

NSC 74859