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説明

Signal transducers and activators of transcription (STATs) are a family of latent cytoplasmic transcription factors that convey signals from the cell membrane to the nucleus. In various human tumors, STAT3 is constitutively activated by aberrant upstream tyrosine kinase activities. Stattic is a small molecule inhibitor of STAT3. It selectively inhibits STAT3 activation, dimerization, and nuclear translocation by preventing the binding of tyrosine-phosphorylated peptide motifs to the STAT3 SH2 domain (IC50 = 5.1 μM at 37°C). At 10 μM, stattic induces apoptosis in STAT3-dependent breast cancer (MDA-MB-231 and MDA-MB-435S) cell lines.