Daminozide
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.
Daminozide,一种植物生长调节剂,选择性地抑制KDM2A、PHF8 和KDM7A ,IC50值分别为1.5 μM、0.55 μM和2 μM [1]。
FBXL11/KDM2A是一种组蛋白H3赖氨酸36去甲基化酶,其酶活性依赖于蛋白质N末端的保守JmjC结构域,该蛋白通过基于羟基化的机制协同铁和α-酮戊二酸催化去甲基化。[2] FBXL11/ KDM2A中的ZF-CxxC DNA结合域可以与非甲基化DNA相互作用,并可以靶向基因组中的CpG岛区域,特异性去除组蛋白H3赖氨酸36甲基化。[3]该机制建立了CpG岛的染色质环境,在大型复杂的哺乳动物的基因组中突出这些调控元件,并将其与非调控区域区分。在一项小鼠肝细胞的研究中,这种基因被证明调节肝糖原异生。[4]
组蛋白Nε甲基赖氨酸去甲基化酶KDM2/7已被鉴定为用于癌症治疗的潜在靶点。肺癌是美国和世界各地癌症死亡的主要原因。非小细胞肺癌(NSCLC)约占所有肺癌病例的85%,其分子病因多样[5]。Klaus W.等人[6]发现NSCLC细胞中KDM2A过表达增加细胞增殖和侵袭性。KDM2A抑制阻断小鼠异种移植模型中的肿瘤生长和NSCLC细胞的侵袭能力,表明KDM2A可能是治疗NSCLC的有希望的靶点。Daminozide,作为一种KDM2A选择性抑制剂,一度被广泛用作植物生长阻滞剂,但现在将是一种靶向治疗NSCLC的有效方法。[7]
参考文献:
1. Nathan R. Rose. et al. Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases. Journal of Medicinal Chemistry. J. Med. Chem. 2012, 55: 66396643.
2. Tsukada Y. et al. "Histone demethylation by a family of JmjC domain-containing proteins". Nature 2006, 439 (7078): 811–6.
3. Blackledge NP. et al. "CpG islands recruit a histone H3 lysine 36 demethylase". Molecular Cell 2010, 38 (2): 179–90..
4. Pan D, Mao C. et al. "The Histone Demethylase Jhdm1a Regulates Hepatic Gluconeogenesis". PLOS Genetics,2012, 8 (6): e1002761.
5. Herbst RS, Heymach JV, Lippman SM. Lung cancer. N Engl J Med. 2008;359(13):1367–1380.
6. Klaus W.et al. KDM2A promotes lung tumorigenesis by epigenetically enhancing ERK1/2 signaling. J Clin Invest. 2013,123(12):5231-5246.
7. Sharma SV, Bell DW, Settleman J, Haber DA. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer. 2007;7(3):169–181.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 160.17 |
Cas No. | 1596-84-5 |
Formula | C6H12N2O3 |
Synonyms | Alar;B 995;DMASA;SADH;Succinic Acid; Aminozide;Kylar;DIMG |
Solubility | ≥16.3 mg/mL in EtOH with gentle warming and ultrasonic; ≥21.4 mg/mL in H2O with gentle warming; ≥7.3 mg/mL in DMSO |
Chemical Name | 4-(2,2-dimethylhydrazinyl)-4-oxobutanoic acid |
SDF | Download SDF |
Canonical SMILES | CN(C)NC(=O)CCC(=O)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。 |
质量控制和MSDS
- 批次: