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Cat. No. Name Size Price Add Cart
KI0266S3I-2015 mg$112
S3I-20110 mg$192
S3I-20150 mg$592

Chemical Characteristic

Product NameS3I-201
SynonymsNSC 74859
CAS No.501919-59-1
Molecular Weight 365.36
FormulaC16H15NO7S
Chemical Name?2-Hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]benzoic acid
SmilesC(=O)(c1c(cc(cc1)NC(=O)COS(=O)(=O)c1ccc(cc1)C)O)O
Chemical Structure

Biological activities

S3I-201 is a chemical probe inhibitor of signal transducer and activator of transcription 3 (STAT3), which effectively inhibits HCC cell growth. [1] S3I-201 inhibits Stat3-Stat3 complex formation and Stat3 DNA-binding with an IC50 of 86 µM, and transcriptional activities. S3I-201 inhibits MDA-MB-231, MDA-MB-435, and MDA-MB-468 cells growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3. In human breast tumor xenograft models, S3I-201 induces growth inhibition and apoptosis of malignant cells in part by constitutively inhibiting active Stat3 and induces human breast tumor regression. At 30-100 µM, S3I-201-induces significant apoptosis in the representative human breast carcinoma cell line MDA-MB-435 and NIH 3T3/v-Src, both of which harbor constitutively active Stat3.[2] In vivo, S3I-201 inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin and inhibits the growth of human breast tumors. S3I-201 inhibits HCC cell proliferation, with the most potent effects with decreased pS727 STAT3 levels and reduces levels of TGF-β pathway proteins. S3I-201 inhibits Huh-7, SNU-398 cells, SNU-475 cells and SNU-182 cells with IC50s of 150, 150, 15 and 200 µM, respectively. S3I-201 inhibits breast carcinoma MDA-MB-435, MDAMB-453 and MDA-MB-231 cell lines with an IC50 close to 100 µM in vitro, but in vivo S3I-201 effectively retards the growth of MDA-MB-231 cells at 5 mg/kg. [3]

Protocols

S3I-201 are prepared in DMSO, stored at -20°C, and diluted in fresh medium for experiment. [1]

References

[1] Hu QD, et al. NSC 74859 enhances doxorubicin cytotoxicity via inhibition of epithelial??esenchymal transition in hepatocellular carcinoma cells. Cancer Lett. 2012, 325(2): 207-213.
[2] Siddiquee K, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Pro Natl Acad Sci. 2007, 104: 7391??396.
[3] Lin L, et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling. Oncogene. 2009, 28(7): 961??72.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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