现货,NSC 74859 (S3I-201),CAS号:501919-59-1,美国进口, JAK / STAT, STAT, STAT 抑制剂和化合物,目录号S1155

信号转导通路: JAK / STAT >> STAT >> STAT 抑制剂 >> NSC 74859 (S3I-201)http://www.selleck.cn/s31-201-S1155.html

技术数据:

分子量(MW): 365.36

化学式:

C16H15NO7S

 

溶解度: DMSO ≥73mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 501919-59-1

生物活性

 

 

NSC 74859 (S3I-201) is a chemical probe inhibitor of Stat3 activity, which was identified from the National Cancer Institute chemical libraries by using structure-based virtual screening with a computer model of the Stat3 SH2 domain bound to its Stat3 phosphotyrosine peptide derived from the x-ray crystal structure of the Stat3 beta homodimer.

S31-201 inhibits Stat3-Stat3 complex formation and Stat3 DNA-binding (IC50 =86±33μM) and transcriptional activities. Furthermore, S31-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3.

Finally, NSC 74859 (S3I-201) inhibits the expression of the Stat3-regulated genes encoding cyclin D1, BcI-xL, and survivin and inhibits the growth of human breast tumors in vivo. Therefore the antitumor activity of S31-201 is mediated in part through inhibition of aberrant Stat3 activation and provide the proof-of-concept for the potential clinical use of Stat3 inhibitors such as S31-201 in tumors harboring aberrant Stat3. [1]

 

 

 

参考文献

Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity Khandaker Siddiquee,Shumin Zhang,et al. PNAS May 1, 2007;104:7391–7396

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