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Description

A cell-permeable naphthol compound that inhibits IL-6-stimulated STAT3 Tyr705 phosphorylation and nuclear translocation in HepG2 cells (IC50 = 73 and 39 µ,M, respectively) by targeting STAT3 SH2 domain peptide-binding pocket (IC50 = 20 µ,M against EGFR-derived pY-peptide binding), while exhibiting little effect against IFN-gamma-stimulated HepG2 cellular STAT1 phosphorylation even at concentrations as high as 300 µ,M. Shown to preferentially induce apoptosis in cultures expressing constitutively active STAT3 (EC50 = 0.73, 3.96, and 7.01 µ,M 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 µ,M in MDA-MB-453 and MCF7 cultures, respectively).