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KU-55933

产品编号 T2685 CAS 587871-26-9

别名: ATM Kinase Inhibitor

KU-55933 (ATM Kinase Inhibitor) 是一种 ATM 抑制剂，IC50和 Ki 值分别为 12.9 和 2.2 nM。它对 ATM 的选择性比对 PI3K/PI4K、 DNA-PK、ATR 和 mTOR 高。

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KU-55933, CAS 587871-26-9

规格	价格/CNY	货期
2 mg	￥ 258	现货
5 mg	￥ 398	现货
10 mg	￥ 578	现货
25 mg	￥ 987	现货
50 mg	￥ 1,660	现货
100 mg	￥ 2,890	现货
1 mL * 10 mM (in DMSO)	￥ 455	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
靶点活性	ATM:12.9 nM
体外活性	ATM抑制剂KU-55933比JAK2抑制剂AG490,或STAT3β的过表达更强烈地影响TRAIL介导的细胞凋亡.KU-55933抑制ATM依赖的STAT3激活,通过上调DR5表达增加TRAIL调节的凋亡,抑制STAT3和NF-κB都和下调cFLIP有关,伴随着凋亡水平上升.
体内活性	KU-55933是ATM有效的特定抑制剂,IC50为13 nM,Ki值为2.2 nM。KU-55933抑制ATM,通过阻断下游TAp63α的激活,提高存活力。KU-55933剂量依赖性抑制ATM依赖的磷酸化作用,IC50为300 nM。KU-55933使HeLa细胞对电离辐射敏感。KU-55933抑制癌细胞增殖。KU-55933抑制癌细胞中生长因子诱导的Akt的磷酸化作用。KU-55933也抑制DNA-PK和PI3K,IC50分别为2.5和16.6 μM。KU-55933也抑制mTOR活性,IC50为9.3 μM。小于30 μM时,KU-58050不能抑制p53的ATM-依赖性磷酸化作用（位点为第15位丝氨酸）。KU-55933的添加对UV-诱导的H2AX（位点为第139位丝氨酸）,NBS1（位点为第343为丝氨酸）,CHK1（位点为第345位丝氨酸）及SMC1（位点为第966位丝氨酸）没有明显作用效果。
激酶实验	Purified enzyme assays: ATM for use in the in vitro assay is obtained from HeLa nuclear extract by immunoprecipitation with rabbit polyclonal antiserum raised to the COOH-terminal 400 amino acids of ATM in buffer containing 25 mM HEPES (pH 7.4), 2 mM MgCl2, 250 mM KCl, 500 μM EDTA, 100 μM Na3VO4, 10% v/v glycerol, and 0.1% v/v Igepal. ATM-antibody complexes are isolated from nuclear extract by incubating with protein A-Sepharose beads for 1 hour and then through centrifugation to recover the beads. In the well of a 96-well plate, ATM-containing Sepharose beads are incubated with 1 μg of substrate glutathione S-transferase–p53N66 (NH2-terminal 66 amino acids of p53 fused to glutathione S-transferase) in ATM assay buffer [25 mM HEPES (pH 7.4), 75 mM NaCl, 3 mM MgCl2, 2 mM MnCl2, 50 μM Na3VO4, 500 μM DTT, and 5% v/v glycerol] at 37 °C in the presence or absence of inhibitor. After 10 minutes with gentle shaking, ATP is added to a final concentration of 50 μM and the reaction continued at 37 °C for an additional 1 hour. The plate is centrifuged at 250 × g for 10 minutes (4 °C) to remove the ATM-containing beads, and the supernatant is removed and transferred to a white opaque 96-well plate and incubated at room temperature for 1.5 hours to allow glutathione S-transferase-p53N66 binding. This plate is then washed with PBS, blotted dry, and analyzed by a standard ELISA technique with a phospho-serine 15 p53 antibody. The detection of phosphorylated glutathione S-transferase-p53N66 substrate is performed in combination with a goat antimouse horseradish peroxidase-conjugated secondary antibody. Enhanced chemiluminescence solution is used to produce a signal and chemiluminescent detection is carried out.
细胞实验	U2OS cells are exposed to ionizing radiation (3, 5, or 15 Gy) or UV (5 or 50 J/m2) and the ATM response determined by Western blot analysis of p53 serine 15 phosphorylation and stabilization of wild-type p53. Whole cell extracts are obtained from each time point, proteins separated by SDS-PAGE, and the ATM-specific increase in phosphorylated serine 15 measured with a p53 phospho-serine 15 specific antibody. Overall p53 stabilization with time is also observed with a p53-specific antibody (DO-1). Similarly, for studying ATM-dependent phosphorylations on H2AX, CHK1, NBS1, and SMC1, the following antibodies are used: CHK1 phospho-serine 345 and NBS1 phospho-serine 343 antibodies. Histone H2A (H-124) and CHK1 antibodies are also used, as well as SMC1 and SMC1 phospho-serine 966 antibodies. For determination of a cellular IC50 for KU-55933, the peak response time for p53 serine 15 phosphorylation of 2 hours is used to monitor inhibition of ATM. KU-55933 is titrated onto cells and preincubated for 1 hour before ionizing radiation. Using scanning densitometry, the percentage inhibition relative to vehicle control is calculated, and the IC50 value is calculated as for the in vitro determinations.(Only for Reference)

别名	ATM Kinase Inhibitor
分子量	395.49
分子式	C21H17NO3S2
CAS No.	587871-26-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 19.8 mg/mL (50 mM)

DMSO: 39.6 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.5285 mL	12.6425 mL	25.2851 mL	63.2127 mL
	5 mM	0.5057 mL	2.5285 mL	5.057 mL	12.6425 mL
	10 mM	0.2529 mL	1.2643 mL	2.5285 mL	6.3213 mL
	20 mM	0.1264 mL	0.6321 mL	1.2643 mL	3.1606 mL
	50 mM	0.0506 mL	0.2529 mL	0.5057 mL	1.2643 mL
DMSO	100 mM	0.0253 mL	0.1264 mL	0.2529 mL	0.6321 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Hickson I, et al. Cancer Res. 2004, 64(24), 9152-9159. 2. Soleimani R, et al. Aging. 2011, 3(8), 782-793. 3. Ivanov VN, et al. Cancer Res. 2009, 69(8), 3510-3519. 4. Hu L, Li B, Chen G, et al. A novel M phase blocker, DCZ3301 enhances the sensitivity of bortezomib in resistant multiple myeloma through DNA damage and mitotic catastrophe. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-14. 5. Huang C Y, Hsieh F S, Wang C Y, et al. Supplementary Methods Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ATM-mediated DNA damage response. EUROPEAN JOURNAL OF CANCER.

文献引用

1. Huang C Y, Hsieh F S, Wang C Y, et al. Supplementary Methods Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ATM-mediated DNA damage response. EUROPEAN JOURNAL OF CANCER. 2019 2. Hu L, Li B, Chen G, et al A novel M phase blocker, DCZ3301 enhances the sensitivity of bortezomib in resistant multiple myeloma through DNA damage and mitotic catastrophe. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-14 3. Bi X, Zhang M, Zhou J, et al.Phosphorylated Hsp27 promotes adriamycin resistance in breast cancer cells through regulating dual phosphorylation of c-Myc.Cellular Signalling.2023: 110913. 4. Yu Z Z, Xu B Q, Wang Y Y, et al.GSK2606414 Sensitizes ABCG2-Overexpressing Multidrug-Resistant Colorectal Cancer Cells to Chemotherapeutic Drugs.Biomedicines.2023, 11(11): 3103. 5. Shen X, Xia Y, Lu H, et al.Synergistic targeting of TrxR1 and ATM/AKT pathway in human colon cancer cells.Biomedicine & Pharmacotherapy.2024, 174: 116507.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

KU-55933 587871-26-9 Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR DNA-PK PI3K mTOR KU55933 Inhibitor inhibit Ataxia telangiectasia mutated KU 55933 ATM and RAD3 related ATM Kinase Inhibitor inhibitor

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KU-55933

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

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