KU 55933
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
KU-55933是一种特异性的ATM激酶抑制剂，IC50值为13 nM[1]。
ATM可以刺激Akt的Ser473磷酸化，介导胰岛素诱导的Akt充分激活。在血清饥饿后用胰岛素和IGF-I处理的MDA-MB-453和PC-3细胞中，作为ATM的抑制剂，KU-55933显著抑制Akt Ser473磷酸化的增加。在MTT实验中，KU-55933在10 μM浓度时抑制约50%的MDA-MB-453和PC-3细胞的增殖。在具有不同Akt活性的细胞系中，KU-55933引起与Akt磷酸化相关的细胞增殖抑制。据报道，在MDA-MB-453和PC-3细胞中，KU-55933也通过下调细胞周期蛋白D1的水平，从而诱导G1期细胞周期停滞[2]。
参考文献：
[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.
- 1. Karin Broennimann, Inna Ricardo-Lax, et al. "RNR-R2 Upregulation by a Short Non-Coding Viral Transcript." Biomolecules. 2021 Dec 3;11(12):1822. PMID:34944466
- 2. Zheng K, Ma J, et al. "Sulforaphane Inhibits Autophagy and Induces Exosome-Mediated Paracrine Senescence via Regulating mTOR/TFE3." Mol Nutr Food Res. 2020;e1901231. PMID:32476238
- 3. Sarkar R, Patra U, et al. "Rotavirus activates a noncanonical ATM-Chk2 branch of DNA damage response during infection to positively regulate viroplasm dynamics." Cell Microbiol. 2019 Dec 17:e13149. PMID:31845505
- 4. Inna Ricardo-Lax, Karin Broennimann, et al. "A short HBV RNA region induces RNR-R2 expression in non-cycling cells and in primary human hepatocytes." bioRxiv. 2018 October 31.
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 395.49 |
| Cas No. | 587871-26-9 |
| Formula | C21H17NO3S2 |
| Solubility | ≥41.67 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 2-morpholin-4-yl-6-thianthren-1-ylpyran-4-one |
| SDF | Download SDF |
| Canonical SMILES | C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
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细胞系 |
MCF-7细胞 |
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制备方法 |
该化合物在DMSO中的溶解度大于10 mM，若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
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反应条件 |
10 μM，72 hours |
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实验结果 |
通过计数能够排除台盼蓝的细胞来测量KU-55933对活细胞数的影响。KU-55933显著减少细胞数量。在KU-55933处理的细胞中，乳酸产生显著增加。KU-55933处理的细胞葡萄糖消耗增加。KU-55933也降低MCF-7细胞中的ATP水平。 |
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注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
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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. |
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| 描述 | KU-55933（ATM激酶抑制剂）是一种有效的和特异性的ATM抑制剂，IC50/Ki值为12.9 nM/2.2 nM，与DNA-PK、PI3K/PI4K、ATR和mTOR相比，对ATM具有高度选择性。 | |||||
| 靶点 | ATM | ATM | ||||
| IC50 | 13 nM | 2.2 nM (Ki) | ||||
质量控制和MSDS
- 批次:
化学结构
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