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KU-55933

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Chemical Structure| 587871-26-9 同义名 : ​ATM Kinase Inhibitor;ATM Kinase Inhibitor
CAS号 : 587871-26-9
货号 : A528135
分子式 : C21H17NO3S2
纯度 : 96%
分子量 : 395.495
MDL号 : MFCD08276985
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(126.42 mM)，配合低频超声助溶，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
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • ATM

    ATM, IC50:12.9 nM
描述 The serine/threonine protein kinase ATM signals can regulate cell cycle and DNA repair components through phosphorylation on the targets such as p53, CHK2, NBS1, and BRCA1, thus playing a central role in the maintenance of genome integrity. KU-55933 is a specific ATM inhibitor with IC50 value of 13nM and Ki value of 2.2nM (measured by ATM kinase activity). After exposure to 5 Gy of irradiation, treatment with 10μM KU-55933 caused increased phosphorylation of p53 at serine 15 site, a marker of ATM activity, in a time-dependent manner in U2OS cells in within 4 hours.

A range of ATM target phosphorylation events, including pH2AX-ser139, pNBS1-ser343, pCHK1-ser345, or pSMC1-ser966, were decreased by pretreatment with 10μM KU-55933 for 1h before irradiation 3Gy or 15Gy in U2OS cells. The radiosensitization by KU-55933 can be observed in HeLa cells pre-treated with 10μM KU-55933 before a range of ionizing radiation (0-4Gy). Also it can sensitize HeLa cells to the cytotoxic effects of the topoisomerase II inhibitors etoposide, doxorubicin, amsacrine and the topoisomerase I inhibitor camptothecin. These suggested that KU-55933 performed as a radio- and chemosensitizer[1].
作用机制 KU-55933 is an ATP-competitive ATM inhibitor.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
639-V Growth Inhibition Assay IC50=27.5119 μM SANGER
697 Growth Inhibition Assay IC50=19.0201 μM SANGER
8305C Growth Inhibition Assay IC50=16.1889 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.28mL

5.06mL

2.53mL
参考文献

[1]Hickson I, Zhao Y, et al. Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer Res. 2004 Dec 15;64(24):9152-9.