BMH-21 是一流的 DNA 嵌入剂，可抑制 RNA 聚合酶 I (Pol I) 转录。 BMH-21 具有抗癌活性。
| Cas No. | 896705-16-1 |
| 化学名 | N-(2-(dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide |
| Canonical SMILES | O=C1C2=C(C=C(C=CC=C3)C3=C2)N=C4C(C(NCCN(C)C)=O)=CC=CN41 |
| 分子式 | C21H20N4O2 |
| 分子量 | 360.41 |
| 溶解度 | ≥ 7.4mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BMH-21 is a planar heterocyclic small molecule DNA intercalator with inhibition of Pol I activity at IC50 = 0.06 µM. [1]
DNA interaction is a well-recognized property for several classes of cancer drugs, which interact with the duplex DNA with three typical binding modalities, namely DNA intercalation, groove binding and covalent interactions. [1]
BMH-21 intercalated into dsDNA and had binding preference towards GC-rich DNA sequences. BMH-21 had wide cytotoxic activities against human cancer cell lines, and acted in p53-independent manner, widely considered as a mediator of many cytotoxic agents. BMH-21 played as a novel agent that inhibited transcription of RNA polymerase I (Pol I) by binding to ribosomal (r) DNA that caused Pol I blockade and degradation of the large catalytic subunit of Pol I, RPA194. BMH-21 led to the dissolution of the nucleolar structure. [1] BMH-21 clearly induced p53 expression in the epithelial compartment of human prostate tissues indicating tissue permeability. [2]
References:
[1]. Colis L, Peltonen K, Sirajuddin P et al. DNA intercalator BMH-21 inhibits RNA polymerase I independent of DNA damage response. Oncotarget. 2014 Jun 30;5(12):4361-9.
[2]. Peltonen K, Colis L, Liu H et al. Identification of novel p53 pathway activating small-molecule compounds reveals unexpected similarities with known therapeutic agents. PLoS One. 2010 Sep 27;5(9):e12996. |
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