Chemical Name : 3-[5-(2-氟苯基)-1,2,4-恶二唑-3-基]苯甲酸
CAS : 775304-57-9
储存条件:Storage at -20C 2 years
S31-201 (NSC 74859) 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 +/- 33uM) and transcriptional activities. Furthermore, S31-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3.Finally, S31-201 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. Siddiquee K et al. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6.