Dp44mT
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.
Dp44mT是铁螯合剂,选择性抑制拓扑异构酶IIα,对人乳腺癌细胞系MDA-MB-231的 GI50值约100 nmol/L[1]。
拓扑异构酶在染色体分离、DNA合成和转录中起重要作用。拓扑异构酶I和拓扑异构酶II是真核生物主要的两大类拓扑异构酶。人类细胞包含拓扑异构酶II的两种同工酶,称为topo IIa和topo IIβ[2]。
在对照实验中,NALM-6白血病top2α+/-细胞中top2α酶的表达大约为野生型细胞的57%。经过100 nmol/L的Dp44mT处理,与top2α+/+细胞相比,top2α+/-细胞对于药物的细胞毒性具有一定抗性。经过100 nmol/L 的Dp44mT 处理,top2α+/+细胞展现了31.7%的sub-G1,而top2α+/-仅为9.4%。在HeLa细胞中,siRNA介导的top2α瞬态降低导致了top2α蛋白质水平减少大约78%。与对照siRNA处理的细胞相比,在top2α siRNA细胞中,在72小时后,0.1和0.3 μmol/L的Dp44mT出现局部抗性[1]。
在体内,0.1和1 μmol/L的Dp44mT治疗6和24小时后,导致DNA和top2α之间共价复合物的形成。没有观察到top1或top2β复合物的形成。Caspase抑制剂预处理没有恢复top2α复合物的形成,因此形成的top2α-DNA复合物不是凋亡的次级效应[1]。
参考文献:
[1]. Rao VA, Klein SR, Agama KK, et al. The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIα in breast cancer cells. Cancer research, 2009, 69(3): 948-957.
[2]. Tan KB, Dorman TE, Falls KM, et al. Topoisomerase IIα and topoisomerase IIβ genes: characterization and mapping to human chromosomes 17 and 3, respectively. Cancer Research, 1992, 52(1): 231-234.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 285.37 |
Cas No. | 152095-12-0 |
Formula | C14H15N5S |
Solubility | ≥62.5 mg/mL in DMSO; insoluble in H2O; ≥22.95 mg/mL in EtOH |
Chemical Name | (Z)-N'-(di(pyridin-2-yl)methylene)-N,N-dimethylcarbamohydrazonothioic acid |
SDF | Download SDF |
Canonical SMILES | CN(/C(S)=N/N=C(C1=CC=CC=N1)\C2=CC=CC=N2)C |
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
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