STAT3-IN-13

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[1].

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Signaling Pathways >> Stem Cell/Wnt >> STAT

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

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]. Apoptosis Analysis[1] Cell Line: 143B cells Concentration: 0, 0.2, 0.5, and 1 μM Incubation Time: 48 hours Result: Increased the percentage of apoptosis rates of 3.4%, 8.7%, 10.7%, and 23.3% at 0, 0.2, 0.5 and 1 μM, respectively. Western Blot Analysis[1] Cell Line: 143B and HOS cells Concentration: 0, 0.2, 0.5 and 1.0 μM Incubation Time: 24 hours Result: Inhibited STAT3 Y705 phosphorylation and downstream target gene expression including Bcl-2 and VEGF, retained good antitumor activities against control tumor cells without STAT3 knockdown.

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]. Animal Model: Nude mice Dosage: 10 and 20 mg/kg Administration: Intraperitoneal injection; twice daily, for 4 weeks Result: Suppressed tumor weight at a dose of 10 mg/kg.

[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.