STAT3-IN-52

STAT3-IN-52 (Compound 9) is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) . It binds to the pY705 site of STAT3 with a Ki of 440 nM, effectively hindering STAT3 phosphorylation and dimerization. STAT3-IN-52 exhibits potent cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 of 0.7 μM), medulloblastoma UW426, and pancreatic cancer BKPC3 cells. The compound induces apoptosis, inhibits STAT3's nuclear translocation and DNA-binding activity, and downregulates the expression of the STAT3 target gene MMP9. STAT3-IN-52 is useful in research related to cancers with aberrant STAT3 activation.