s3i-201

Description: S3I-201 (also called S3I201; NSC74859; S3I 201; NSC-74859) is a cell permeable and selective Stat3 inhibitor with potential anticancer activity. It inhibits Stat3 with an IC50 of 86+/-33 uM. S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 uM in cell-free assays, and exhibits low activity towards STAT1 and STAT5. 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 uM. 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 uM, respectively.

References: Proc Natl Acad Sci U S A. 2007 May 1; 104(18):7391-6; Proc Natl Acad Sci U S A. 2012 Jan 10; 109(2):600-5.