3076446-44-8
Chemical Structure
Topobexin
- CAS No.: 3076446-44-8
- Formula:C29H35N3O4
- Molecular Weight:489.61
InChIKey: LNTXOIHSBUUKNJ-UHFFFAOYSA-N
SMILES: CCCC1=CC(OC2=C(C(OCCN3CCN(CC3)C)=CC=C12)C(N4CCCC5=C4C=CC=C5)=O)=O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Topobexin | 99.04% | 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. | ||||||||||||||||||||
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- [1]. Kubeš J, et al. Topobexin targets the Topoisomerase II ATPase domain for beta isoform-selective inhibition and anthracycline cardioprotection. Nat Commun. 2025;16(1):4928. Published 2025 May 28. [Content Brief]
- [2]. Kosić M, et al. Drug Repositioning in Doxorubicin-Induced Cardiotoxicity Protection. Int J Mol Sci. 2025;26(20):10130. Published 2025 Oct 17. [Content Brief]
- [3]. Veronika Kerestes, et al. Analysis of Gene Expression Changes upon Topobexin Treatment and TOP2B-knockout in hiPSC derived cardiomyocytes. bioRxiv. March 11, 2026.
Keywords
