BMH-21 is a potent small molecule DNA intercalator. BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription. BMH-21 does not cause phosphorylation of H2AX, a key biomarker activated in DNA damage stress. 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. The findings also show that interference with DNA and DNA metabolic processes can be exploited therapeutically without causing DNA damage.
Chemical Formula: C21H22N4O2
Exact Mass: 362.1743
Molecular Weight: 362.43
Elemental Analysis: C, 69.59; H, 6.12; N, 15.46; O, 8.83
Chemical Name: N-(2-(dimethylamino)ethyl)-12-oxo-11a,12-dihydro-5aH-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
InChi Code: InChI=1S/C21H22N4O2/c1-24(2)11-9-22-20(26)16-8-5-10-25-19(16)23-18-13-15-7-4-3-6-14(15)12-17(18)21(25)27/h3-8,10,12-13,17-18H,9,11H2,1-2H3,(H,22,26)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
BMH-21 inhibits RNA polymerase I independent of DNA damage response.
BMH-21 inhibits 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 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences.
BMH-21 (1 μM; 3 h ours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation.
BMH-21 (50 mg/kg; i.p.; daily, for 6 days) inhibits HCT116 colon cancer tumor growth in vivo.
Colis L, Peltonen K, Sirajuddin P, Liu H, Sanders S, Ernst G, Barrow JC, Laiho M. DNA intercalator BMH-21 inhibits RNA polymerase I independent of DNA damage response. Oncotarget. 2014 Jun 30;5(12):4361-9. PubMed PMID: 24952786; PubMed Central PMCID: PMC4147329.
Colis L, Ernst G, Sanders S, Liu H, Sirajuddin P, Peltonen K, DePasquale M, Barrow JC, Laiho M. Design, synthesis, and structure-activity relationships of pyridoquinazolinecarboxamides as RNA polymerase I inhibitors. J Med Chem. 2014 Jun 12;57(11):4950-61. doi: 10.1021/jm5004842. Epub 2014 May 30. PubMed PMID: 24847734; PubMed Central PMCID: PMC4059246.
Peltonen K, Colis L, Liu H, Trivedi R, Moubarek MS, Moore HM, Bai B, Rudek MA, Bieberich CJ, Laiho M. A targeting modality for destruction of RNA polymerase I that possesses anticancer activity. Cancer Cell. 2014 Jan 13;25(1):77-90. doi: 10.1016/j.ccr.2013.12.009. PubMed PMID: 24434211; PubMed Central PMCID: PMC3930145.
Products are for research use only. Not for human use.
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