STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research.
STAT3-IN-13 (compound 6f) (48 hours) has anti-proliferative activity with IC50 values of 0.25, 0.11 and 0.55 μM for 143B, HOS and MG63 cells, respectively[1].STAT3-IN-13 (compound 6f) (0.001-100 μM) binds to STAT3 and interacts with STAT3586−685 in a concentration dependent manner with a KD of 0.96 μM[1].STAT3-IN-13 (compound 6f) (0-1.0 μM; 24 hours; 143B and HOS cells) inhibits STAT3 Y705 phosphorylation and suppresses STAT3 in tumor cells[1].STAT3-IN-13 (compound 6f) (0-1.0 μM; 48 hours; 143B cells) induces apoptosis in a dose-dependent manner[1].
STAT3-IN-13 (compound 6f) (10-20 mg/kg; i.p.; twice daily, for 4 weeks; nude mice) blocks osteosarcoma growth and metastasis in vivo[1].
References:
[1]. Jin W, et, al. Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis. J Med Chem. 2022 May 12;65(9):6710-6728.