Background:

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

inS3-54A18 (5 μM) reduces wound healing to 64% and 76% for A549 and MDA-MB-231 cells, respectively. inS3-54A18 at 10 μM further reduces the healing to 47% and 39%, respectively. inS3-54A18 inhibits the expression of STAT3 downstream target genes and the binding of STAT3 to its endogenous target sequences. inS3-54A18 does not affect the constitutive or IL-6-induced STAT3 activation (Tyr705 phosphorylation) but represses STAT3 target gene (survivin) expression[1].

inS3-54A18 (200 mg/kg, p.o.) inhibits tumor growth, metastasis and expression of STAT3 target genes in a mouse xenograft model of A549 cells[1].

[1]. Huang W, et al. Small-molecule inhibitors targeting the DNA-binding domain of STAT3 suppress tumor growth, metastasis and STAT3 target gene expression in vivo. Oncogene. 2016 Feb 11;35(6):783-92