TargetMol

Merbarone

Product Code:
 
TAR-T28017
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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Further Information

Bioactivity:
Merbarone is a Type II DNA topoisomerase inhibitor. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. Merbarone induces activation of caspase-activated DNase and excision of chromosomal DNA loops from the nuclear matrix. Merbarone induces apoptosis in CEM cells through activation of ICE/CED-3-like protease.
CAS:
97534-21-9
Formula:
C11H9N3O3S
Molecular Weight:
263.27
Purity:
0.98
SMILES:
O=CN(C1C(=O)NC(=S)NC1=O)c1ccccc1

References

1. Spallarossa A, Rotolo C, Sissi C, Marson G, Greco ML, Ranise A, La Colla P, Busonera B, Loddo R. Further SAR studies on bicyclic basic merbarone analogues as potent antiproliferative agents. Bioorg Med Chem. 2013 Nov 1;21(21):6328-36. doi: 10.1016/j.bmc.2013.08.056. PubMed PMID: 24063907. 2. Pastor N, Dom?nguez I, Orta ML, Campanella C, Mateos S, Cort?s F. The DNA topoisomerase II catalytic inhibitor merbarone is genotoxic and induces endoreduplication. Mutat Res. 2012 Oct-Nov;738-739:45-51. doi: 10.1016/j.mrfmmm.2012.07.005. PubMed PMID: 22921906. 3. Attia SM. Dominant lethal mutations of topoisomerase II inhibitors etoposide and merbarone in male mice: a mechanistic study. Arch Toxicol. 2012 May;86(5):725-31. doi: 10.1007/s00204-011-0799-6. PubMed PMID: 22207148. 4. Wang L, Roy SK, Eastmond DA. Differential cell cycle-specificity for chromosomal damage induced by merbarone and etoposide in V79 cells. Mutat Res. 2007 Mar 1;616(1-2):70-82. PubMed PMID: 17174356.