2361304-26-7
2361304-26-7 结构式
基本信息
STAT3 inhibitor 3
2H-1-Benzopyran-2-one, 3-[[4-[(4-bromo-1,1-dioxidobenzo[b]thien-2-yl)carbonyl]-1-piperazinyl]carbonyl]-7-(diethylamino)-
物理化学性质
常见问题列表
|
STAT3
|
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 IC
50
s 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. |
STAT3-IN-3 (10mg/kg-20 mg/kg; i.p.; daily; for 14 days) possesses potent antitumor activity against implanted 4T1 breast tumors growth.
| Animal Model: | Adult female BALB/c mice (6 weeks of age) |
| Dosage: | 10 mg/kg, 20 mg/kg |
| Administration: | Intraperitoneal injection, daily, for 14 days |
| Result: | Significantly inhibited tumor volume. |