Dp44mT
(Synonyms: 2-(二-2-吡啶基亚甲基)-N,N-二甲基肼基硫代甲酰胺) 目录号 : GC15399
An iron chelator with antiproliferative effects
Cas No.:152095-12-0
Sample solution is provided at 25 µL, 10mM.
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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.
Kinase experiment: | For DNA topoisomerase IIα assays, the 161-bp fragment from pBluescript SK(-) phagemid DNA or single stranded oligonucleotides are 5'-end labeled with [32P]ATP and T4 polynucleotide kinase. Labeling mixtures are subsequently centrifuged through Mini Quick Spin DNA columns (for pSK fragments) or Oligo columns (for oligonucleotides) to remove the unincorporated label. Annealing to the complementary strand of the oligonucleotides is done by heating the reaction mixture to 95°C and overnight cooling to room temperature in 10 mM Tris-HCl (pH 7.8), 100 mM NaCl, and 1 mM EDTA. DNA substrates (10 pmol/reaction) are incubated with 500 ng of top2a or top2h in the presence or absence of Dp44mT for the indicated times at 25°C in 10 μL of reaction buffer. Reactions are stopped by adding SDS (final concentration 0.5%). Samples are separated on 16% (for pSK DNA) or 20% (for the oligonucleotides) denaturing polyacrylamide gels (7 M urea). Imaging and quantitation are done using a PhosphorImager[1]. |
Cell experiment: | Cell proliferation is measured using a sulforhodamine B dye–based assay. MDA-MB-231(breast cancer) and MCF-12A (healthy mammary epithelial) cells are incubated with increasing concentrations of Dp44mT (0.01, 0.1, 1, 10, 100 μM). Results are expressed relative to control[1]. |
References: [1]. Rao VA, et al. The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIalpha in breast cancer cells. Cancer Res. 2009 Feb 1;69(3):948-57. | |
| Cas No. | 152095-12-0 | SDF | |
| 别名 | 2-(二-2-吡啶基亚甲基)-N,N-二甲基肼基硫代甲酰胺 | ||
| 化学名 | (Z)-N'-(di(pyridin-2-yl)methylene)-N,N-dimethylcarbamohydrazonothioic acid | ||
| Canonical SMILES | CN(/C(S)=N/N=C(C1=CC=CC=N1)\C2=CC=CC=N2)C | ||
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5042 mL | 17.5211 mL | 35.0422 mL |
| 5 mM | 0.7008 mL | 3.5042 mL | 7.0084 mL |
| 10 mM | 0.3504 mL | 1.7521 mL | 3.5042 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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