Biological Activity
Selectively inhibits STAT3 DNA-binding activity in vitro (IC50 values are 86, 160, and >300 μM for STAT3-STAT3, STAT1-STAT3 and STAT1-STAT1 DNA-binding activity respectively). Blocks growth and induces apoptosis preferentially in tumor cells that contain persistently active STAT3 in vitro and arrests tumor growth in a murine xenograft model in vivo.
Compound Libraries
NSC 74859 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 365.36 |
| Formula | C16H15NO7S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 501919-59-1 |
| PubChem ID | 252682 |
| InChI Key | HWNUSGNZBAISFM-UHFFFAOYSA-N |
| Smiles | CC1=CC=C(S(OCC(NC2=CC=C(C(O)=O)C(O)=C2)=O)(=O)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 365.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.74 mL | 13.69 mL | 27.37 mL |
| 5 mM | 0.55 mL | 2.74 mL | 5.47 mL |
| 10 mM | 0.27 mL | 1.37 mL | 2.74 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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References
References are publications that support the products' biological activity.
Lin et al (2009) The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-beta signaling. Oncogene 28 961 PMID: 19137011
Siddiquee et al (2007) Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc.Natl.Acad.Sci.U.S.A. 104 7391 PMID: 17463090
Keywords: NSC 74859, supplier, NSC74859, STAT3, inhibitors, inhibits, DNA-binding, apoptosis, S3I-201, STAT, STAT, Tocris Bioscience
