STAT3-IN-10 是一种STAT3抑制剂，IC50为 5.18 μM。STAT3-IN-10 与STAT3 SH2结构域直接结合，抑制肿瘤细胞生长和诱导肿瘤细胞的凋亡 (apoptosis)。
| 生物活性 | STAT3-IN-10 is aSTAT3inhibitor with anIC50value of 5.18 μM. STAT3-IN-10 directly binds toSTAT3SH2domain, inducescancercellsapoptosis[1]. |
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体外研究
(In Vitro) | STAT3-IN-10 (A11) (48 h) shows IC50values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively[1].
STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain[1].
STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells[1].
Cell Viability Assay[1] | Cell Line: | Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2. | | Concentration: | | | Incubation Time: | 48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2). | | Result: | Showed IC50values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | MDA-MB-231. | | Concentration: | 0, 0.75, 1.5 and 3.0 μM. | | Incubation Time: | 24 h. | | Result: | Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701. |
Apoptosis Analysis[1] | Cell Line: | MDA-MB-231. | | Concentration: | 0, 1, 2, and 4 μM. | | Incubation Time: | 24 h. | | Result: | Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner |
Cell Cycle Analysis[1] | Cell Line: | MDA-MB-231. | | Concentration: | 0, 1, 2, and 4 μM. | | Incubation Time: | 24 h. | | Result: | Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells |
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体内研究
(In Vivo) | STAT3-IN-10 (A11) (i.p.; 5, 10 mg/kg; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo[1].
| Animal Model: | Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231[1]. | | Dosage: | 5 and 10 mg/kg | | Administration: | IP, once a day, 21 days | | Result: | Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
