WR-S-462 is a highly potent and selective STAT3 inhibitor with SPR Kd of 58 nM, directly interferes with the STAT3-SH2 domain interaction.
WR-S-462 significantly disrupts STAT3 nuclear localization and inhibits STAT3 Y705 phosphorylation both in MDA-MB-231 and BT549 cells.
WR-S-462 exhibits little inhibitory effects on JAK1, JAK2, JAK3, EGFR, and SRC kinases, shows no discernible impact on the phosphorylation levels of JAK1, ERK1/2, AKT, STAT1, and STAT5.
WR-S-462 selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells.
WR-S-462 strongly suppresses the colony formation of TNBC cells.
WR-S-462 forcefully suppresses the migration and invasion of TNBC cells.
WR-S-462 promotes TNBC cell apoptosis, inhibits tumor growth in preclinical TNBC xenografts.
