Molecular Formula | C16H15NO7S |
Molar Mass | 365.36 |
Density | 1.507 |
Melting Point | >185oC (dec.) |
Boling Point | 654.7±55.0 °C(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 2.98±0.10(Predicted) |
Storage Condition | -20°C |
MDL | MFCD09907564 |
Use | S3I-201 |
In vitro study | S3I-201 selectively inhibits Stat3 DNA binding activity. S3I-201 inhibits the complex form of Stat3 · Stat3, independent of the activation state of STAT3. S3I-201 does not interfere with the binding of Lck SH2 to the homologous pTyr peptide. S3I-201 action on NIH 3T3/v-Src murine fibroblasts and human breast cancer MDA-MB-231, MDA-MB-435, and MDA-MB-468 cells inhibits Stat3 activation. S3I-201 inhibits stat3-dependent transcriptional activity. S3I-201 also inhibited the expression of stat3-regulated genes encoding cyclin D1, Bcl-xL, and survival. S3I-201 can reduce pS727STAT3 levels and reduce TGF-beta pathway protein levels. S3I-201 also inhibited CD133 and CD133 − Huh-7 cells. The latest study shows that S3I-201 acts on Hep-G2, Huh-7 and SK-HEP-1 cells, potentiating the antiproliferative effects of Cetuximab. |
In vivo study | 5 mg/kg dose of S3I-201 in mice carrying human breast cancer (MDA-MB-231), showed a strong inhibitory effect. S3I-201 at a dose of 5 mg/kg showed strong anticancer activity in the Huh-7 xenograft tumor, with no significant external health changes or weight loss symptoms. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.737 ml | 13.685 ml | 27.37 ml |
5 mM | 0.547 ml | 2.737 ml | 5.474 ml |
10 mM | 0.274 ml | 1.369 ml | 2.737 ml |
5 mM | 0.055 ml | 0.274 ml | 0.547 ml |
biological activity | S3I-201 effectively inhibited fstat3 DNA binding activity, IC50 was 86 μm, and the inhibition of STAT1 and STAT5 was weak. S3I-201 (NSC 74859) effectively inhibited the DNA binding activity of STAT3 with an IC50 of 86 μm, while the inhibitory activity against STAT1 and STAT5 was low. |
features | S3I-201 is a chemical detector inhibitor that removes breast tumors. |
Target | Value |
STAT3 (Cell-free assay) | 86 μM |