STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC 50 of 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 induces apoptosis
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. antiproliferative activity (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: SF-767, PrEC cells Concentration: 0-40 µM Incubation Time: 6 h Result: Showed cytotoxicity in a dose dependent manner. Western Blot AnalysisCell 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 AnalysisCell 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.
