产品属性：
产品名称 | 规格 | CAS号 | 型号 |
Dp44mT | 10mM (in 1mL DMSO) 10mg 50mg 200mg | 152095-12-0 | EY-Y0165348 |
Cas No.152095-12-0
别名
化学名 (Z)-N'-(di(pyridin-2-yl)methylene)-N,N-dimethylcarbamohydrazonothioic acid
分子式 C14H15N5S
分子量 285.37
溶解度 ≥ 62.5mg/mL in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
Dp44mT is an iron chelator that selectively inhibit topoisomerase IIα, with an GI50 value of ~100 nmol/L in the human breast cancer cell line MDA-MB-231 [1].
Topoisomerases play important roles in chromosome segregation, DNA synthesis, and transcription. Topoisomerase I and topoisomerase II are two major types of topoisomerases in eukaryotes. Human cells contain two isozymes of topoisomerase II, named topo IIa and topo IIβ [2].
In control experiments, the Nalm-6 leukemic top2α+/- cells expressed ~57% as much levels of top2α enzyme as the wild type cells. Treated with Dp44mT at 100 nmol/L, compared with the top2α+/+ cells, top2α+/- cells showed partial resistance to the cytotoxic effects of the drug.After the exposure to Dp44mT at 100 nmol/L, the top2α+/+ cells showed 31.7%, while the top2α+/- cells only showed 9.4% sub-G1 containing cells. In HeLa cells, transient siRNA-mediated knockdown of top2α resulted in a reduction of ~78% in the protein level for top2α. In top2α siRNA cells, a partial resistance to Dp44mT (0.1 and 0.3 µmol/L) was found at 72 hours, compared with the control siRNA-treated cells [1].
In vivo, 6 and 24 hours after the treatment with 0.1 and 1 µmol/L of Dp44mT, the treatment resulted in the covalent complex formation between DNA and top2α. No complex formation was found after the treatment when probed for top1 or top2β. Caspase inhibitor pretreatment did not rescue the formation of top2α complex, so the formed top2α-DNA complexes were not the secondary effect of apoptosis [1].
References:
[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.
关键字： 152095-12-0;C14H15N5S;Dp44mT;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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