BMH-21

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BMH-21  纯度: 98.61%

BMH-21是一种首创的 DNA 嵌入剂 (DNA intercalator)，可抑制 RNA 聚合酶 I (Pol I) 转录。BMH-21 具有抗癌活性。

BMH-21

BMH-21 Chemical Structure

CAS No. : 896705-16-1

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BMH-21 相关产品

•相关化合物库:

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  • Anti-Aging Compound Library

生物活性

BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity[1][2].

IC50 & Target

DNA[1][2]
体外研究
(In Vitro)

BMH-21 binds ribosomal DNA and inhibits Pol I transcription[1].
BMH-21 inhibits RNA polymerase I independent of DNA damage response[1].
BMH-21 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences[1].
BMH-21 (1 μM; 3 hours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: U2OS cells
Concentration: 0 μM, 0.1 μM , 1 μM, 10 μM
Incubation Time: 48 hours
Result: Decreased the viability of cells at concentrations that activated the DNA damage response.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 1 μM
Incubation Time: 3 hours
Result: Degraded RPA194 with blocked ATM and DNA-PKcs activity.

体内研究
(In Vivo)

BMH-21 (50 mg/kg; i.p.; daily; for 6 days) inhibits HCT116 colon cancer tumor growth in vivo[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week old athymic NCr nu/nu mice, with HCT116 colorectal carcinoma xenograft[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection, daily, for 6 days
Result: Significantly inhibited HCT116 colon cancer tumor growth.

分子量

360.41

Formula

C21H20N4O2
CAS 号

896705-16-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 1 mg/mL (2.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7746 mL 13.8731 mL 27.7462 mL
5 mM — — —
10 mM — — —

*

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。-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。
参考文献

  • [1]. Colis L, et al. DNA intercalator BMH-21 inhibits RNA polymerase I independent of DNA damage response. Oncotarget. 2014 Jun 30;5(12):4361-9.

    [2]. Karita Peltonen, et al. A Targeting Modality for Destruction of RNA Polymerase I that Possesses Anticancer Activity. Cancer Cell. 2014 Jan 13; 25(1): 77–90.

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