NSC 74859
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NSC 74859(S3I-201 )是一种选择性的Stat3抑制剂,IC50值为86 μM。
体外的Stat3 DNA结合实验表明,S3I-201能够有效地抑制Stat3的DNA结合活性,平均IC50值为86 μM。EMSA实验表明,S3I-201能够选择性地抑制Stat3的DNA结合活性,大于对Stat1和Stat5 DNA结合活性的抑制。S3I-201能够抑制Stat1-Stat3和Stat1-Stat1复合物的形成,IC50值分别为160和>300 μM。此外,S3I-201所抑制的Stat3的DNA结合活性能够被未磷酸化和未激活状态的Stat3单体修复。这说明S3I-201的抑制作用不依赖于激活状态。在NIH 3T3/v-Src成纤维细胞中,S3I-201能够抑制Stat3的组成型激活,并降低pTyr-705 Stat3的水平。另外,在浓度为30-100 μM时,S3I-201能够显著诱导具有组成性激活Stat3的细胞凋亡。S3I-201还可以减少这些细胞中细胞周期蛋白D1、Bcl-xL和surviving的表达。
参考文献:
[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.
- 1. Qi Yuan, Jianchun Gu, et al. "MyD88 in myofibroblasts enhances colitis-associated tumorigenesis via promoting macrophage M2 polarization." Cell Rep. 2021 Feb 2;34(5):108724. PMID:33535045
- 2. 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
- 3. 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
- 4. 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
- 5. 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
- 6. Marie R.Mooney."Precision Medicine Approaches to Integrating Genomics with Cancer Therapy: Applications in Glioblastoma and Lymphoma." ProQuest LLC. 2016.
Storage | Store at -20°C |
M.Wt | 365.36 |
Cas No. | 501919-59-1 |
Formula | C16H15NO7S |
Synonyms | S3I-201;NSC74859;NSC-74859;S3I 201 |
Solubility | insoluble in H2O; ≥18.25 mg/mL in DMSO; ≥2.2 mg/mL in EtOH with gentle warming |
Chemical Name | 2-hydroxy-4-[[2-(4-methylphenyl)sulfonyloxyacetyl]amino]benzoic acid |
SDF | Download SDF |
Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |
质量控制和MSDS
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