BMH 21

Names

[ Name ]:
BMH 21

[Synonym ]:
N-[2-(Dimethylamino)ethyl]-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
12H-Benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide, N-[2-(dimethylamino)ethyl]-12-oxo-
BMH-21
BMH21

Biological Activity

[Description]:

BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.IC50 value: 10-90 nM(RPA195 IC50) [1]Target: RNA Pol I inhibitorin vitro: BMH-21 effects on the nucleolar stress response were independent of major DNA damage associated PI3-kinase pathways, ATM, ATR and DNA-PKcs. BMH-21 is a chemically unique DNA intercalator that has high bioactivity towards Pol I inhibition without activation or dependence of DNA damage stress [1].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Research Areas >> Cancer

[References]

[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]. Colis L, et al. Design, synthesis, and structure-activity relationships of pyridoquinazolinecarboxamides as RNA polymerase I inhibitors. J Med Chem. 2014 Jun 12;57(11):4950-61.

[3]. Peltonen K, et al. Small molecule BMH-compounds that inhibit RNA polymerase I and cause nucleolar stress. Mol Cancer Ther. 2014 Nov;13(11):2537-46.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₁H₂₀N₄O₂

[ Molecular Weight ]:
360.409

[ Exact Mass ]:
360.158630

[ PSA ]:
66.71000

[ LogP ]:
1.57

[ Appearance of Characters ]:
light yellow to dark yellow

[ Index of Refraction ]:
1.668

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: soluble1mg/mL, clear (warmed)

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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