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• 产品描述： 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

• 靶点： DNA-PK:14 nM (IC50);mTOR:1.7 μM (IC50);PI3K:5.0 μM (IC50);CRISPR/Cas9 ;DNA-PK;CRISPR/Cas9

• 体内研究：
  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. 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. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage

• 参考文献：
  1. Justin J J Leahy, et al. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. 2. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905 3. Hardcastle IR, et al. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. J Med Chem. 2005 Dec 1;48(24):7829-46 4. Ember SW, et al. The acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem Biol. 2014 Feb 25. 5. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93

• 溶解性： DMSO  :  14.29  mg/mL  (34.56  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.418 ml	12.092 ml	24.184 ml
  5 mM	0.484 ml	2.418 ml	4.837 ml
  10 mM	0.242 ml	1.209 ml	2.418 ml
  50 mM	0.048 ml	0.242 ml	0.484 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *