Merbarone, A cell-permeable anticancer drug that inhibits the catalytic activity of topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes.
A cell-permeable anticancer drug that inhibits the catalytic activity of topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes (IC50 = 20 µM for purified mammalian topo II versus IC50 = ~ 200 µM for topo I). Also induces apoptosis in human leukemic CEM cells through a caspase-3-like protease-dependent mechanism.
A cell-permeable, anticancer drug that inhibits the catalytic activity of DNA topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes (IC50 = 20 µM for purified mammalian topoisomerase II versus IC50 ~200 µM for topoisomerase I). Also induces apoptosis in human leukemic CEM cells through a caspase-3-like protease-dependent mechanism.
Biochem/physiol Actions
Cell permeable: yes
Primary Target Catalytic activity of topoisomerase II
Product does not compete with ATP.
Reversible: no
Target IC50: 20 µM for purified topoisomerase II (topo II)
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Khelifa, T., and Beck, W.T. 1999. Mol. Pharmacol. 55, 548. Drake, F.H., et al. 1989. Cancer Res.49, 2578. Brewer, A.D., et al. 1985. Biochem. Pharmacol.34, 2047.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Topoisomerase II (Topo II) is essential for mitosis since it resolves sister chromatid catenations. Topo II dysfunction promotes aneuploidy and drives cancer. To protect from aneuploidy, cells possess mechanisms to delay anaphase onset when Topo II is perturbed, providing additional
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