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Nanaomycin A
Nanaomycin A 是第一个选择性 DNMT3B 抑制剂,IC50 为 500 nM。Nanaomycin A 是一种醌类抗生素,可重新激活人类癌细胞中沉默的抑癌基因。Nanaomycin A 抑制人疟原虫恶性疟原虫的体外生长,IC80 值为 33.1 nM
目录号: PC10115 纯度: ≥98%
CAS No. :52934-83-5
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PC10115-5mg 5mg ¥3430.00 请登录
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PC10115-10mM (in 1mL DMSO) 10mM(in1mLDMSO) ¥3332.00 请登录
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中文名称
Nanaomycin A
中文别名
七尾霉素
英文名称
Nanaomycin A
英文别名
1H-Naphtho[2,3-c]pyran-3-aceticacid, 3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-, (1S,3R)-;2-[(1S,3R)-9-hydroxy-1-methyl-5,10-dioxo-3,4-dihydro-1H-benzo[g]isochromen-3-yl]acetic acid;4-deoxykalafunginic acid;CHEBI:48202;dihydrokalafungin;Nanafrocin;Nanafrocin [INN];Nanafrocina [Spanish];Nanafrocine;Nanafrocine [French];Nanafrocinum;Nanafrocinum [Latin];Nanaomycin A;Rosanomycin A;Antibiotic OS 3966A;Nanafrocin;NNM-A;NSC 267461
Cas No.
52934-83-5
分子式
C16H14O6
分子量
302.28
包装储存
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
生物活性
Nanaomycin A is a quinone bacterial metabolite originally isolated from Streptomyces that has antimicrobial activity.1 It inhibits the growth of a variety of bacteria (MICs = <0.01-1.56 µg/ml), fungi (MICs = 0.4-3.12 µg/ml), and plant pathogenic fungi (MICs = 0.4-12.5 µg/ml), as well as P. falciparum (IC80 = 0.033 µM).1,2 Nanaomycin A is a selective DNA methyltransferase 3B (DNMT3B) inhibitor that inhibits proliferation of HCT116, A549, and HL-60 cancer cells (IC50s = 0.4, 4.1, and 0.8 µM, respectively).3 Nanaomycin A promotes the differentiation of human induced pluripotent stem (iPS) cells into hepatoblasts at the definitive endoderm cell-to-hepatoblast stage, but not the iPS cell-to-definitive endoderm cell stage, when used at a concentration of 1 µM.
性状
Solid
IC50 & Target[1][2]

DNMT3B

500 nM (IC50)

Plasmodium

 

体外研究(In Vitro)

Nanaomycin A (10-10000 nM; 72 hours) has a distinct cytotoxic effect in all three cell lines.
Nanaomycin A (0.5, 5 μM; 72 hours) reveals induction of RASSF1A protein expression in A549 cells.
Nanaomycin A (5 μM; 72 hours) has an 18-fold relative induction.
Nanaomycin A not affects the enzymatic activity of DNMT1.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

Cell Line: HCT116 (colon), A549 (lung), and HL60 (bone marrow) human tumor cell lines
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 72 hours
Result: Had a distinct cytotoxic effect in all three cell lines.

Western Blot Analysis

Cell Line: A549 cells
Concentration: 0.5, 5 μM
Incubation Time: 72 hours
Result: Revealed induction of RASSF1A protein expression.

RT-PCR

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 72 hours
Result: Had an 18-fold relative induction.
运输条件
Room temperature or refrigerated transportation.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
1. Iwai, Y., Kimura, K., Takahashi, Y., et al. OM-173, new nanaomycin-type antibiotics produced by a strain of Streptomyces. Taxonomy, production, isolation and biological properties. J. Antibiot. (Tokyo) 36(10), 1268-1274 (1983).
2. Tanaka, T., Kamei, K., Otoguro, K., et al. Heme-dependent radical generation: Possible involvement in antimalarial action of non-peroxide microbial metabolites, nanaomycin A and radicicol. J. Antibiot. (Tokyo) 52(10), 880-888 (1999).
3. Kuck, D., Caulfield, T., Lyko, F., et al. Nanaomycin A selectively inhibits DNMT3B and reactivates silenced tumor suppressor genes in human cancer cells. Mol. Cancer Ther. 9(11), 3015-3023 (2010).
4. Nakamae, S., Toba, Y., Takayama, K., et al. Nanaomycin A treatment promotes hepatoblast differentiation from human induced pluripotent stem cells. Stem Cells Dev. 27(6), 405-414 (2018).
溶解度数据
体外研究: 

DMSO : 100 mg/mL (330.82 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3082 mL 16.5410 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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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