DM-01

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DM-01  纯度: 98.03%

DM-01 是一种强效的选择性 EZH2 抑制剂，可用于弥漫性大 B 细胞淋巴瘤 (DLBCL)，滤泡性淋巴瘤 (FL) 和 SNF5/INI-1/SMARCB1 基因相关实体瘤的研究。

DM-01

DM-01 Chemical Structure

CAS No. : 2355280-00-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
50 mg ￥13000 In-stock
100 mg ￥20000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

DM-01 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].

IC50 & Target[1]

EZH2

 

体外研究
(In Vitro)

Knockdown EZH2 in A549 cells results in the decrease of cell sensitivity to DM-01 at 50 and 100 μM concentrations. DM-01 also shows comparable inhibitory activity for K562 cells with an IC50 value of 58.706 μΜ[1].
DM-01 (5 and 10 μM; 24 hours) strongly inhibits the activity of EZH2 and results in abolished H3K27me expression in K562 cells[1].
DM-01 (5 and 10 μM) also increases the transcription expression of DIRAS3 in a dose dependent manner, a tumor suppressor in downstream of EZH2[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549 sh-EV and A549 sh-EZH2 cells
Concentration: 1, 5, 10, 50, 100 μM
Incubation Time: 48 hours
Result: The IC50s of 72.748 and 269.7 μΜ for A549 sh-EV and A549 sh-EZH2 cells, respectively.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 5, 10 μM
Incubation Time: 24 hours
Result: Inhibited the activity of EZH2 and resulted in abolished H3K27me expression.

分子量

431.45

Formula

C23H24F3N3O2
CAS 号

2355280-00-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (115.89 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3178 mL 11.5888 mL 23.1777 mL
5 mM 0.4636 mL 2.3178 mL 4.6355 mL
10 mM 0.2318 mL 1.1589 mL 2.3178 mL

*

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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Qifan Zhou, et al. Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents. New Journal of Chemistry. 10 Jan 2020.

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