S3I-201 (NSC74859) is a cell-permeable, amidosalicylic acid based small molecule that inhibits Stat3 activity with IC50 of 86 µM1. S3I-201 binds to the Stat3-SH2 domain and prevents its dimerization, inhibiting stat3 phosphorylation, translocation and Stat3-dependent transcription activities. S31-201 preferentially inhibits growth and induces apoptosis in tumor cells that contain persistently activated stat31. In addition, S3I-201 has been shown to retard stat3-dependent tumor growth in human breast tumor xenograft models, and to impair VZV infection of skin xenografts in vivo1,2,3.
Technical information:
| Chemical Formula: | C16H15NO7 S | |
| CAS #: | 501919-59-1 | |
| Molecular Weight: | 365.36 | |
| Purity: | >98% | |
| Appearance: | Off white solid | |
| Chemical Name: | 2-Hydroxy-4-[[[(4-methylphenyl)sulfonyloxy]acetyl]amino]-benzoic acid | |
| Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Siddiquee K. 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):7391-6. |
| 2. | Lin L, et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-beta signaling. Oncogene, 2009, 28(7), 961-972. |
| 3. | Sen N, et al. Signal transducer and activator of transcription 3 (STAT3) and survivin induction by varicella-zoster virus promote replication and skin pathogenesis. Proc Natl Acad Sci U S A, 2012, 109(2), 600-605. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
