Nanaomycin A
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.
Nanaomycin A是一个选择性的DNA甲基转移酶3B(DNMT3B)抑制剂,IC50值为500 nM [1]。
在体外甲基化实验中,Nanaomycin A选择性地抑制DNMT3B而非DNMT1,尽管Nanaomycin A以多步骤对接的方法停靠在人DNMT1的催化域上。在HCT116、A549和HL60细胞中,Nanaomycin A抑制细胞活力,IC50值分别为400 nM、4100 nM和800 nM。此外,Nanaomycin A显著降低了这些细胞的基因组甲基化水平。在A549细胞中,Nanaomycin A处理导致RASSF1A启动子的去甲基化。Nanaomycin A引起的去甲基化重新激活了被甲基化沉默的肿瘤抑制基因的转录和表达[1]。
参考文献:
[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.
- 1. Daehwan Kim, Subin Kim, et al. "Autologous treatment for ALS with implication for broad neuroprotection." Transl Neurodegener. 2022 Mar 11;11(1):16. PMID: 35272709
- 2. Liu PY, Sokolowski N, et al. "The BET bromodomain inhibitor exerts the most potent synergistic anticancer effects with quinone-containing compounds and anti-microtubule drugs." Oncotarget. 2016 Nov 29;7(48):79217-79232. PMID: 27764794
- 3. Nicolson SC, Li C, et al. "Identification and validation of small molecules that enhance recombinant Adeno-associated virus transduction following high throughput screen." J Virol. 2016 May 4. pii: JVI.02953-15. PMID: 27147738
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 302.28 |
Cas No. | 52934-83-5 |
Formula | C16H14O6 |
Synonyms | Nanafrocin, Nanafrocine, Nanafrocinum, Rosanomycin A |
Solubility | insoluble in H2O; ≥15.1 mg/mL in DMSO; ≥31.07 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-[(1S,3S)-9-hydroxy-1-methyl-5,10-dioxo-3,4-dihydro-1H-benzo[g]isochromen-3-yl]acetic acid |
SDF | Download SDF |
Canonical SMILES | OC1=CC=CC(C(C2=C3[C@H](C)O[C@H](CC(O)=O)C2)=O)=C1C3=O |
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]: | |
细胞系 |
A549、HL60、HeLa和HCT116细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
10 nM ~ 10 μM;72 h |
应用 |
Nanaomycin A最初是通过DNMT1抑制剂的虚拟筛选而鉴定得到的,在来自不同组织的三个不同肿瘤细胞系中均具有抗增殖活性。在三个细胞系中,nanaomycin A减少整体甲基化水平,激活RASSF1A肿瘤抑制基因的转录。在生化试验中,nanaomycin A对DNMT3B具有选择性。 |
动物实验[2]: | |
动物模型 |
豚鼠 |
应用 |
评估nanaomycin A和siccanin对豚鼠中实验性皮肤癣菌(Trichophyton mentagrophytes)感染的治疗效果。Nanaomycin A的局部使用可以有效改善病变情况,阻止感染组织真菌的生长。Nanaomycin A和siccanin在实验中具有可比的活性。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
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 |
描述 | Nanaomycin A是一个选择性的DNMT3B抑制剂。 | |||||
靶点 | DNMT3B | |||||
IC50 | 500 nM |
质量控制和MSDS
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