STAT3-IN-3 has no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2.
STAT3-IN-3 inhibits the growth of MDA-MB-231, HCT-116, HepG2, and MCF-7 cells with IC50s of 1.43 μM, 1.89 μM, 2.88 μM, and 3.33 μM, respectively.
STAT3-IN-3 down-regulates the expression of STAT3 target genes Bcl-2 and Cyclin D1.
STAT3-IN-3 inhibits STAT3 tyrosine phosphorylation and serine phosphorylation.
STAT3-IN-3 inhibits STAT3 DNA-binding activity.
STAT3-IN-3 (1-4 μM; 24 hours) increases ROS production and remarkably reduces the mitochondrial membrane potential to induce mitochondrial apoptotic pathway.
STAT3-IN-3 (1-4 μM; 24 hours) can induce the cleavage of caspase-9, caspase-3 and PARP.
Cell Viability Assay
| Cell Line: |
MDA-MB-231 cells, HCT-116 cells, HepG2 cells, MCF-7cells |
| Concentration: |
MTT assay |
| Incubation Time: |
48 hours |
| Result: |
Exhibited anti-proliferative activity. |
Apoptosis Analysis
| Cell Line: |
MDA-MB-231 cells |
| Concentration: |
0 μM, 1 μM, 2 μM, 4 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced the apoptosis of MDA-MB-231 cells dose-dependently and the apoptosis rates. |
Western Blot Analysis
| Cell Line: |
MDA-MB-231 cells |
| Concentration: |
0 μM, 1 μM, 2 μM, 4 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced the cleavage of caspase-9, caspase-3 and PARP. |