Topobexin is a selective inhibitor of Topoisomerase II beta (TOP2B), demonstrating an IC50 value of 0.19 μM for TOP2B and 4.8 μM for TOP2A in DNA decatenation assays. By binding to non-homologous residues within the obex pocket, Topobexin effectively targets the ATPase domain of TOP2B. This compound mitigates anthracycline-induced DNA double-strand breaks and associated apoptotic signaling without impairing the anticancer effects of anthracyclines in cancer cells. It serves as a valuable tool for research into anthracycline-induced cardiotoxicity, revealing insights into cellular stress responses and cardiac function.
Topobexin is a selective inhibitor of Topoisomerase II beta (TOP2B), demonstrating an IC50 value of 0.19 μM for TOP2B and 4.8 μM for TOP2A in DNA decatenation assays. By binding to non-homologous residues within the obex pocket, Topobexin effectively targets the ATPase domain of TOP2B. This compound mitigates anthracycline-induced DNA double-strand breaks and associated apoptotic signaling without impairing the anticancer effects of anthracyclines in cancer cells. It serves as a valuable tool for research into anthracycline-induced cardiotoxicity, revealing insights into cellular stress responses and cardiac function.
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