STAT3-SH2 domain inhibitor 1 是一种有效的 Src 同源性 2 (SH2) STAT3结构域 (STAT3-SH2 domain) 抑制剂，其Kd值为1.57 μM。STAT3-SH2 domain inhibitor 1 可抑制 STAT3 信号转导和转录激活。STAT3-SH2 domain inhibitor 1 诱导胃癌细胞凋亡 (apoptosis)。STAT3-SH2 domain inhibitor 1 可用于癌症的研究。
| 生物活性 | STAT3-SH2 domain inhibitor 1 is a potentSrcHomology 2 (SH2) Domain ofSTAT3(STAT3-SH2 domain)inhibitor with aKdvalue of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibitsSTAT3signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 inducesapoptosisin gastriccancercells. STAT3-SH2 domain inhibitor 1 can be used in research ofcancer[1]. |
体外研究
(In Vitro) | STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway[1].
STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively[1].
STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells[1].
Cell Viability Assay[1] | Cell Line: | AGS and MGC-803 cell lines | | Concentration: | 0-10 μM | | Incubation Time: | 72 hours | | Result: | Suppressed cancer cell proliferation and growth. |
Apoptosis Analysis[1] | Cell Line: | AGS and MGC-803 cell lines | | Concentration: | 1 and 3 μM | | Incubation Time: | 72 hours | | Result: | Induced apoptosis in AGS cells in a concentration-dependent manner, resulting in apoptotic percentages of 13.0 and 26.7% at 1 and 3 μM, respectively.
Induced apoptosis of MGC-803 cells in a dose-dependent way, leading to apoptotic percentage of 11.2% at 5 μM.
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Western Blot Analysis[1] | Cell Line: | AGS and MGC-803 cell lines | | Concentration: | 1 and 3 μM | | Incubation Time: | 24 hours | | Result: | Inhibited STAT3 phosphorylation at Tyr705 in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | HEK-293T cells | | Concentration: | 1, 3, and 5 μM | | Incubation Time: | 24 hours | | Result: | Disrupted STAT3 dimerization in HEK-293T cells. |
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体内研究
(In Vivo) | STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts[1].
| Animal Model: | BALB/c male nude mice with gastric tumor xenografts[1] | | Dosage: | 5 and 15 mg/kg | | Administration: | Intraperitoneal injection; daily, for 20 days | | Result: | Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of
65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively. |
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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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