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DC-05

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Chemical Structure| 890643-16-0 同义名 : DC_05
CAS号 : 890643-16-0
货号 : A221717
分子式 : C25H25N3O
纯度 : 98+%
分子量 : 383.486
MDL号 : MFCD08236399
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(273.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 DNA methyltransferases are responsible for catalyzing the methylation of adenine/cytosine residues in specific regions of the genome, and they participate in the establishment of epigenetic modification patterns. Deregulation of DNA methyltransferase activity will disturb DNA methylation systems, leading to the occurrence of various human diseases including cancers[2] DNA methyltransferase inhibitors have been approved for the treatment of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myelogenous leukemia[3].DNA methylation is one of the most important epigenetic modifications often occurring on the cytosine of CpG islands located in gene promoter regions, which is thought to be closely correlated with tumorigenesis[4].DNA methylation and histone deacetylation are key epigenetic processes involved in normal cellular function and tumorigenesis. Therapeutic strategies based on DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors are currently in use and under development for the treatment of cancers[5].DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively. DC-05 shows less potent activities against DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9, and PRMT1 (IC50: >200, >200, >150, >150, >150, >150, 37.1 μM). DC-05 (1.25, 2.5, 5, and 10 μM) potently inhibits the proliferation of HCT116 (human colon cancer) and Capan-1 (human pancreatic adenocarcinoma cells) after treatment for 24, 48, and 72 h[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL
参考文献

[1]Chen S, Wang Y, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-41.

[2]Fei Ma ,et al. Nanomaterial-based biosensors for DNA methyltransferase assay. J Mater Chem B. 2020 Apr 29;8(16):3488-3501.

[3]Elodie M Da Costa,et al. DNA Methylation-Targeted Drugs. Cancer J. Sep/Oct 2017;23(5):270-276.

[4]Xiao-Yun Lü,et al. Application of DNA methyltransferase inhibitors for myelodysplastic syndrome. Yi Chuan. 2013 Feb;35(2):136-40.

[5]S R Teixeira,et al. Direct monitoring of breast and endometrial cancer cell epigenetic response to DNA methyltransferase and histone deacetylase inhibitors. Biosens Bioelectron. 2019 Sep 15;141:111386.

[6] Chen S, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-41.