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。
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.
性状
Solid
IC50 & Target[1][2]
DNA
体外研究(In Vitro)
BMH-21 binds ribosomal DNA and inhibits Pol I transcription.BMH-21 inhibits RNA polymerase I independent of DNA damage response.BMH-21 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences.BMH-21 (1 μM; 3 hours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: 6-week old athymic NCr nu/nu mice
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
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.
溶解度数据
In Vitro: DMSO : 1 mg/mL (2.77 mM; Need ultrasonic)配制储备液