Brief Description

NSC 74859(S3I-201) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM, and low activity towards STAT1 and STAT5.
IC50 value: 86 uM
Target: STAT3
NSC 74859 (S3I-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. 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 NSC 74859 (S31-201) in tumors harboring aberrant Stat3.
References on NSC 74859:
[1]. Khandaker Siddiquee 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): 7391-7396. L Lin et al. The STAT3 inhibitor NSC 748
[2]. L Lin et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling Oncogene (2009) 28, 961-972
[3]. Hu QD, Chen W, Yan TL, Ma T, Chen CL, Liang C, Zhang Q, Xia XF, Liu H, Zhi X, Zheng XX, Bai XL, Yu XZ, Liang TB. NSC 74859 enhances doxorubicin cytotoxicity via inhibition of epithelial-mesenchymal transition in hepatocellular carcinoma cells. Cancer Lett. 2012 Jul 7.
[4]. Chen W, Shen X, Xia X, Xu G, Ma T, Bai X, Liang T. NSC 74859-mediated inhibition of STAT3 enhances the anti-proliferative activity of cetuximab in hepatocellular carcinoma. Liver Int. 2012 Jan;32(1):70-7. doi: 10.1111/j.1478-3231.2011.02631.x.

Solubility

in DMSO > 10 mM

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid