KU 55933
(Synonyms: 2-吗啉-4-基-6-噻蒽-1-基吡喃-4-酮) 目录号 : GC11118
An ATM kinase inhibitor
Cas No.:587871-26-9
Sample solution is provided at 25 µL, 10mM.
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KU-55933 is a specific inhibitor of ATM kinase with IC50 value of 13 nM [1].
ATM can stimulate Ser473 phosphorylation of Akt and mediate its full activation in response to insulin. As an ATM inhibitor, KU-55933 significantly inhibited the increase of phospho-Akt at Ser473 in MDA-MB-453 and PC-3 cells treated with insulin and IGF-I following serum starvation. In the MTT assay, KU-55933 treatment suppressed cell proliferation by about 50% at concentration of 10 μM in MDA-MB-453 and PC-3 cells. In a panel of cell lines that have varied Akt activities, KU-55933 treatment caused cell proliferation inhibition correlated with the Akt phosphorylation. KU-55933 was also found to induce G1 cell cycle arrest through down-regulating the cyclin D1 level in MDA-MB-453 and PC-3 cells [2].
References:
[1] Hickson I, Zhao Y, Richardson C J, et al. Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer research, 2004, 64(24): 9152-9159.
[2] Li Y, Yang D Q. The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Molecular cancer therapeutics, 2010, 9(1): 113-125.
| Cell experiment: [1] | |
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Cell lines |
MCF-7 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
10 μM, 72 hours |
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Applications |
The effect of KU-55933 on viable cell number was measured by counting cells able to exclude Trypan blue. Cell number was significantly reduced by KU-55933. Lactate production was significantly increased in cells treated with KU-55933. Glucose consumption was increased with exposure to KU-55933 treated cells. KU-55933 also decreased ATP levels in MCF-7 cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Zakikhani M, Bazile M, Hashemi S, et al. Alterations in cellular energy metabolism associated with the antiproliferative effects of the ATM inhibitor KU-55933 and with metformin. PloS one, 2012, 7(11): e49513. | |
| Cas No. | 587871-26-9 | SDF | |
| 别名 | 2-吗啉-4-基-6-噻蒽-1-基吡喃-4-酮 | ||
| 化学名 | 2-morpholin-4-yl-6-thianthren-1-ylpyran-4-one | ||
| Canonical SMILES | C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4 | ||
| 分子式 | C21H17NO3S2 | 分子量 | 395.49 |
| 溶解度 | ≥ 41.7mg/mL in DMSO with gentle warming | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5285 mL | 12.6425 mL | 25.2851 mL |
| 5 mM | 0.5057 mL | 2.5285 mL | 5.057 mL |
| 10 mM | 0.2529 mL | 1.2643 mL | 2.5285 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet