Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 µM and 4.8 µM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity[1][2][3].
Molecular Weight:
489.61
Purity:
99.04
CAS Number:
[3076446-44-8]
Formula:
C29H35N3O4
Target:
Topoisomerase
Application Notes:
MCE Product type: Reference compound
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