Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA . Amsacrine isethionate induces Ca 2+ -mediated inactivation of ERK , and also downregulates AKT , promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3 . Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA . Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.
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