573125
STAT3 Inhibitor IX, Cpd188
4-((3-(Carboxymethylsulfanyl)-4-hydroxy-1-naphthyl)sulfamoyl)benzoic acid
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Merck KGaA
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01 June 2012
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A cell-permeable naphthol compound that inhibits IL-6-stimulated STAT3 Tyr705 phosphorylation and nuclear translocation in HepG2 cells (IC50 = 73 and 39 µM, respectively) by targeting STAT3 SH2 domain peptide-binding pocket (IC50 = 20 µM against EGFR-derived pY-peptide binding), while exhibiting little effect against IFN-γ-stimulated HepG2 cellular STAT1 phosphorylation even at concentrations as high as 300 µM. Shown to preferentially induce apoptosis in cultures expressing constitutively active STAT3 (EC50 = 0.73, 3.96, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively), while being less effective against cells without constitutively active STAT3 (EC50 = 15.5 and 17.19 µM in MDA-MB-453 and MCF7 cultures, respectively).
| Product information | |||
|---|---|---|---|
| Form | Beige solid | ||
| Molar mass | 433.5 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C19H15NO7S2 | ||
| CAS number | 823828-18-8 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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