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Description

A cell-permeable oxadiazolyl-quinolinecarboxamide that is shown to selectively suppress STAT3, but not STAT1, STAT5a, or STAT5b, DNA binding activity in nuclear extract from IL-6-stimulated MDA-MB-468 cells (by 74% at 50 microM) and prevent IL-6-stimulated STAT3 dimerization in HEK293 cells (by 50% and 99%, respectively, at 74 and 100 microM), as well as inhibit the expression of STAT3 target genes, c-myc, cyclin D1, and survivin, both in cultures in vitro (effective conc. 50 microM) and in SCC3-derived tumors in mice in vivo (160 mg/kg/day, p.o.)., A cell-permeable oxadiazolyl-quinolinecarboxamide that is shown to selectively suppress STAT3, but not STAT1, STAT5a, or STAT5b, DNA binding activity and prevent IL-6-stimulated STAT3 dimerization in HEK293 cells (by 99% at 100 microM), as well as inhibit the expression of STAT3 target genes both in cultures in vitro (effective conc. 50 microM) and in SCC3-derived tumors in mice in vivo (160 mg/kg/day, p.o.).