Product Name :
BMH-21
Description:
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.
CAS:
896705-16-1
Molecular Weight:
362.42
Formula:
C21H22N4O2
Chemical Name:
N-(2-(dimethylamino)ethyl)-12-oxo-11a,12-dihydro-5aH-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
Smiles :
CN(C)CCNC(=O)C1=CC=CN2C1=NC1C=C3C=CC=CC3=CC1C2=O
InChiKey:
FSCFXXLAGKOPMP-UHFFFAOYSA-N
InChi :
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥360 days if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 896705-16-1|Molecular Weight: 362.42|Formula: C21H22N4O2|Synonym:|BMH21|BMH 21|BMH-21|Chemical Name: N-(2-(dimethylamino)ethyl)-12-oxo-11a,12-dihydro-5aH-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide|Smiles: CN(C)CCNC(=O)C1=CC=CN2C1=NC1C=C3C=CC=CC3=CC1C2=O|InChiKey: FSCFXXLAGKOPMP-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Ivacaftor} site|{Ivacaftor} Autophagy|{Ivacaftor} Protocol|{Ivacaftor} In Vivo|{Ivacaftor} manufacturer|{Ivacaftor} Epigenetic Reader Domain} |Drug Formulation: To be determined.{{Danicopan} site|{Danicopan} Complement System|{Danicopan} Purity & Documentation|{Danicopan} References|{Danicopan} custom synthesis|{Danicopan} Epigenetic Reader Domain} |HS Tariff Code: 382200|How to use|In Vitro:|BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.PMID:35567400 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.|In Vivo:|BMH-21 (50 mg/kg; i.p.; daily, for 6 days) inhibits HCT116 colon cancer tumor growth in vivo.|References:|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.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.|