Description
InS3-54A18 is an active analog of inS3-54 targeting the DBD of STAT3 with IC50 of 8.8uM in STAT3-dependent luciferase reporter assay, with increased specificity and pharmacological properties; not only binds directly to the DBD and inhibits the DNA-binding activity of STAT3 both in vitro and in situ but also effectively inhibits the constitutive and IL-6-stimulated expression of STAT3 downstream target genes; InS3-54A18 is completely soluble in an oral formulation and effectively inhibits lung xenograft tumor growth and metastasis with little adverse effect on animals