| In Vitro |
STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells[1]. STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) [1]. STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a concentration-dependent manner[1]. STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner[1]. STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) [1]. STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner[1]. Cell Cytotoxicity Assay[1] Cell Line: MDA-MB-231 cells Concentration: 20 μM Incubation Time: 48 hours Result: The antiproliferative activity reached 97.86%. Cell Cytotoxicity Assay[1] Cell Line: MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells Concentration: 20 μM Incubation Time: 48 hours Result: Inhibited with IC50 values of 6.01, 7.20, 7.02, 26.54, 25.69 and 12.52 μM for MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells, respectively. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5,5 and 10 μM Incubation Time: 6 hours Result: Decrease the level of p-STAT3 at site pTyr705 in a concentration dependent manner. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5,5 and 10 μM Incubation Time: 6 hours Result: Down-regulated the level of STAT3 downstream genes. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 5, 10 and 15 μM Incubation Time: 48 hours Result: The percentage of apoptotic cells was 24.4% at a concentration of 15 μM.
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