STL127705 (C09-1169-554)

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 apoptosisIn VitroSTL127705 (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.Form:SolidIC50& Target:IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS). Specification: ≥98.0% Molecular Formula: C22H20FN5O4 Molecular Weight: 437.42 PubChem CID: 53333307 Isomeric SMILES: COC1=C(C=C(C=C1)CCNC2=NC=C3C(=N2)NC(=O)N(C3=O)C4=CC(=CC=C4)F)OC