Network Version
KU-57788 Data Sheet
| Product Name: | KU-57788 |
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|---|---|---|
| CAS No.: | 503468-95-9 | |
| Cat. No.: | HY-11006 | |
| MWt: | 413.49 | |
| Formula: | C25H19NO3S | |
| Purity : | >98% | |
| Solubility: | DMSO : 6.67 mg/mL (ultrasonic;warming;heat to 60°C) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| 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]. | ||
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