KU-0060648

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Chemical Structure| 881375-00-4 同义名 : -
CAS号 : 881375-00-4
货号 : A571046
分子式 : C33H34N4O4S
纯度 : 98%
分子量 : 582.71
MDL号 : MFCD17214218
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(3.43 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:0.59 μM

  • p110β

    PI3Kβ, IC50:0.5 nM

  • p110α

    PI3Kα, IC50:4 nM

  • p110δ

    PI3Kδ, IC50:0.1 nM

  • DNA-PK

    DNA-PK, IC50:5 nM
描述 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, and with less inhibition of PI3Kγ with IC50 of 0.59 μM.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human HeLa cells Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50=0.136 μM 23855836
MO59J-Fus1 cells 1 μM Function assay Inhibition of human DNA-PK autophosphorylation at S2056 in MO59J-Fus1 cells at 1 uM 23855836
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.58mL

1.72mL

0.86mL

17.16mL

3.43mL

1.72mL
参考文献

[1]Mao M, Liu Y, et al. Feedback autophagy activation as a key resistance factor of Ku-0060648 in colorectal cancer cells. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1244-1249.

[2]Chen MB, Zhou ZT, et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Oncotarget. 2016 Mar 29;7(13):17047-59.