Nanaomycin A
(Synonyms: 七尾霉素,Nanafrocin, Nanafrocine, Nanafrocinum, Rosanomycin A) 目录号 : GC14562
A bacterial metabolite
Cas No.:52934-83-5
Sample solution is provided at 25 µL, 10mM.
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Nanaomycin A is a selective inhibitor of DNA methyltransferase 3B (DNMT3B) with IC50 value of 500 nM [1].
In the biochemical in vitro methylation assay, Nanaomycin A showed selective inhibition of DNMT3B but not DNMT1 although it was docked to the catalytic domain of human DNMT1 in a multi-step docking approach. Nanaomycin A showed cell viability inhibition in HCT116, A549 and HL60 cells with IC50 values of 400 nM, 4100 nM and 800 nM, respectively. It decreased the genomic methylation level of these cells significantly. Besides that, Nanaomycin A treatment resulted in demethylation of the RASSF1A promoter in A549 cells. The demethylation caused by Nanaomycin A reactivated the transcription and expression of a silenced tumor suppressor gene [1].
References:
[1] Kuck D, Caulfield T, Lyko F, et al. Nanaomycin A selectively inhibits DNMT3B and reactivates silenced tumor suppressor genes in human cancer cells. Molecular cancer therapeutics, 2010, 9(11): 3015-3023.
| Cell experiment[1]: | |
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Cell lines |
A549, HL60, HeLa and HCT116 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 |
Ranging from 10 nM to 10 μM for 72 h |
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Applications |
Nanaomycin A, initially identified by a virtual screening for inhibitors against DNMT1, as a compound inducing antiproliferative effects in three different tumor cell lines originating from different tissues. Nanaomycin A treatment reduced the global methylation levels in all three cell lines and reactivated transcription of the RASSF1A tumor suppressor gene. In biochemical assays, nanaomycin A revealed selectivity toward DNMT3B. |
| Animal experiment [2]: | |
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Animal models |
Guinea pigs |
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Applications |
The therapeutic effect of nanaomycin A and siccanin against experimental cutaneous Trichophyton mentagrophytes infection in guinea pigs was investigated. Topically applied formulation of nanaomycin A was very effective in improving the condition of lesions and in preventing fungal growth in the infected tissues. Nanaomycin A and siccanin were comparable in activity in experiments. |
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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. Kuck D1, Caulfield T, Lyko F et al. Nanaomycin A selectively inhibits DNMT3B and reactivates silenced tumor suppressor genes in human cancer cells. Mol Cancer Ther. 2010 Nov;9(11):3015-23. 2. Kitaura K, Araki Y, Marumo H. The therapeutic effect of nanaomycin A against experimental Trichophyton mentagrophytes infection in guinea pigs. Kitaura K, Araki Y, Marumo H. |
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| Cas No. | 52934-83-5 | SDF | |
| 别名 | 七尾霉素,Nanafrocin, Nanafrocine, Nanafrocinum, Rosanomycin A | ||
| 化学名 | 2-[(1S,3R)-9-hydroxy-1-methyl-5,10-dioxo-3,4-dihydro-1H-benzo[g]isochromen-3-yl]acetic acid | ||
| Canonical SMILES | CC1C2=C(CC(O1)CC(=O)O)C(=O)C3=C(C2=O)C(=CC=C3)O | ||
| 分子式 | C16H14O6 | 分子量 | 302.28 |
| 溶解度 | ≥ 15.1mg/mL in DMSO, ≥ 31.07 mg/mL in EtOH with ultrasonic | 储存条件 | Store 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 | 3.3082 mL | 16.541 mL | 33.0819 mL |
| 5 mM | 0.6616 mL | 3.3082 mL | 6.6164 mL |
| 10 mM | 0.3308 mL | 1.6541 mL | 3.3082 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet