STL127705

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

STL127705 是一种有效的 Ku 70/80 异二聚体蛋白抑制剂，可抑制 Ku70/80-DNA 相互作用，IC50 为 3.5 μM。 STL127705 抑制 Ku 依赖性 DNA-PKCS 激酶的激活，IC50 为 2.5 μM。

STL127705 is a potent Ku 70/80 heterodimer protein inhibitor and inhibits Ku70/80-DNA interaction with IC50 of 3.5 μM. STL127705 inhibits the activation of Ku-dependent DNA-PKCS kinase with IC50 of 2.5 μM.

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.?STL127705 (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells.STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner.TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine. Cell Viability Assay 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 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 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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Compound L | 7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

Cell Cycle/DNA Damage

DNA-PK

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1326852-06-5

437.431

C22H20FN5O4

>98% (HPLC)

In Vitro:?DMSO : 2.4 mg/mL (5.49 mM)

COc1ccc(CCNc2ncc3c(n2)[nH]c(=O)n(-c2cccc(F)c2)c3=O)cc1OC

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(-20℃)

With Ice Pack

≥ 2 years