NU7441 (KU57788)

Description: NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive inhibitor of DNA-PK (DNA-dependent protein kinase) with IC50 of 14 nM, has anticancer activity. It also inhibits PI3K with IC50 value of 5 uM in cell-free assays. NU7441 showed no inhibition effect on the DNA-PK-related enzymes ATM and ATR at concentration of 100 uM. For mTOR and PI3K, NU7441 exhibited inhibition activities with IC50 values of 1.7 and 5 uM, respectively, which were about 100-fold higher than the IC50 value of DNA-PK. NU7441 sensitized HeLa cells to ionizing radiation in vitro, with dose modification factors of 2.5 at 10% survival being observed at 0.5 microM.

References: J Med Chem. 2005 Dec 1; 48(24):7829-46; Cancer Res. 2006 May 15; 66(10):5354-62.