C188-9 (TTI-101) is a novel small-molecule STAT3 inhibitor with Ki of 12.4 nM.
C188-9 inhibits STAT3 binding to its pY-peptide ligand, suppresses cytokine-stimulated pSTAT3, reduces constitutive pSTAT3 activity, and inhibits anchorage dependent and independent growth of in multiple HNSCC cell lines.
C188-9 prevents tumor xenograft growth, modulates many STAT3-regulated genes involved in oncogenesis and radioresistance in vivo.
