DC-05

A non-nucleoside DNMT1 inhibitor

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库存: 现货

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数量
2mg

￥2512.00

2010.00

- +
5mg

￥3737.00

2990.00

- +
10mg

￥5350.00

4280.00

- +
50mg

￥15887.00

12710.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce50538
CAS: 890643-16-0
别名:
分子式: C25H25N3O
分子量: 383.49
纯度: >98%
溶解度: DMSO : 100 mg/mL (260.76 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1; IC₅₀ = 10.3 ?M).¹ It is selective for DNMT1 over DNMT3A and DNMT3B (IC₅₀s = >200 ?M), as well as the additional methyltransferases G9a, SUV39H1, MLL1, SET7/9, and PRMT1 (IC₅₀s = >150, >150, >150, >150, and 37.1 ?M, respectively). DC-05 (2.5-10 ?M) reduces proliferation of HCT116 colon cancer cells.

1.Chen, S., Wang, Y., Zhou, W., et al.Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screeningJ. Med. Chem.57(21)9028-9041(2014)

Protocol

Kinase experiment:

To measure the effects of DC-05 on mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200 μM of DC-05 and S-adenosylmethionine (AdoMet) in the DNMT assay buffer in the assay plate at 37°C for 2 h. Next, every sample is incubated with the capture and detection antibody, followed by incubation with developer solution for 10 min at room temperature. The absorbance is measured at 450 nm using a microplate reader. S-Adenosylhomocysteine (AdoHcy) is used as a positive control[1].

参考文献:

[1]. 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.