STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白Ku 70/80 heterodimer protein抑制剂，IC50为 3.5 μM。STL127705 通过抑制 DNA-PKCS 激酶的激活干扰 Ku70/80 与 DNA 的结合。STL127705 显示出抗增殖和抗肿瘤活性。 STL127705 诱导细胞凋亡 (apoptosis) 。
| 生物活性 | STL127705 (Compound L) is a potentKu 70/80 heterodimer proteininhibitor with anIC50of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 inducesapoptosis[1][2]. |
| IC50& Target | IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS)[1] |
体外研究
(In Vitro) | STL127705 (Compound L) (0-100 μM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase[1].
antiproliferative activity (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells[1].
STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner[1].
TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine[2].
Cell Viability Assay[1] | Cell Line: | SF-767, PrEC cells | | Concentration: | 0-40 μM | | Incubation Time: | 6 h | | Result: | Showed cytotoxicity in a dose dependent manner. |
Western Blot Analysis[1] | Cell Line: | SF-767 cells | | Concentration: | 0-100 μM | | Incubation Time: | pre-treated for 2 h and then co-incubation 4 h | | Result: | Decreased the DNA-PKCS autophosphorylation but total DNA-PKCS was not suppressed by STL127705. |
Apoptosis Analysis[1] | Cell Line: | H1299 cells | | Concentration: | 1 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis with apoptosis rate significantly increased to 76% when treated with STL127705 in combination with gemcitabine. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 2.4 mg/mL(5.49 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) *STL127705 is usually formulated as a suspension. 配制储备液 | 1 mM | 2.2861 mL | 11.4307 mL | 22.8613 mL | | 5 mM | 0.4572 mL | 2.2861 mL | 4.5723 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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