STL127705

Research use only, not for human use.

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 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.

——

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

——

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years