STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 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[1][2].
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].
[1]. Weterings E, et al. A novel small molecule inhibitor of the DNA repair protein Ku70/80. DNA Repair (Amst). 2016 Jul;43:98-106.
[2]. Guo N, et al. Inhibiting nonhomologous end-joining repair would promote the antitumor activity of gemcitabine in nonsmall cell lung cancer cell lines. Anticancer Drugs. 2022 Jun 1;33(5):502-508.