KU-57788

KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC₅₀ of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC₅₀s of 5.0 and 1.7 μM, respectively^[1]. IC50 & Target: IC50: 13 nM (DNA-PK)^[3], 1 μM (BRD4), 3.5 μM (BRDT)^[4] In Vitro: NU7441 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. NU7441 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of NU7441 and 60Coγ IR affects DNA damage repair^[2]. NU7441 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor^[4]. NU7441 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage^[5]. In Vivo: KU-57788 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. KU-57788 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of KU-57788 and 60Coγ IR affects DNA damage repair^[2]. KU-57788 weakly inhibits BRD4 and BRDT with IC₅₀s of 1 μM and 3.5 μM, respectively. KU-57788 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor^[4]. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage^[5].