STAT3-IN-13 (compound 6f) 是一种有效的STAT3抑制剂。STAT3-IN-13 具有抗增殖作用，并以 0.46 μM 的KD值与 STAT3 SH2 结构域结合。STAT3-IN-13 抑制 STAT3 Y705 的磷酸化和下游靶基因表达。STAT3-IN-13 在体外诱导细胞凋亡 (apoptosis)，在体内抑制肿瘤的生长和转移。STAT3-IN-13 可用于癌症研究。
| 生物活性 | STAT3-IN-13 (compound 6f) is a potentSTAT3inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to theSTAT3SH2 domain with a KDof 0.46 μM. STAT3-IN-13 inhibits the phosphorylation ofSTAT3Y705 and downstream target gene expression. STAT3-IN-13 inducesapoptosisin vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used forcancerresearch[1]. |
体外研究
(In Vitro) | STAT3-IN-13 (compound 6f) (48 hours) has anti-proliferative activity with IC50values 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 STAT3586–685in a concentration dependent manner with a KDof 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. |
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体内研究
(In Vivo) | 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. |
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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. |
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