80277-14-1
Chemical Structure
Amsacrine isethionate
Synonym(s): m-AMSA isethionate; Acridinyl anisidide isethionate
- CAS No.: 80277-14-1
- Formula:C23H25N3O7S2
- Molecular Weight:519.59
InChIKey: MZLUSXXMFJMTRB-UHFFFAOYSA-N
SMILES: O=S(O)(CCO)=O.O=S(NC1=CC=C(C(OC)=C1)NC2=C3C=CC=CC3=NC4=C2C=CC=C4)(C)=O
Biological Activity: Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca2+-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[1][2][3][4].
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Amsacrine isethionate | Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca2+-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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- [1]. Lee YC, et al. Amsacrine-induced apoptosis of human leukemia U937 cells is mediated by the inhibition of AKT- and ERK-induced stabilization of MCL1. Apoptosis : an international journal on programmed cell death. 2017 Mar;22(3):406-420. [Content Brief]
- [2]. Thomas D, et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action. British journal of pharmacology. 2004 Jun;142(3):485-94. [Content Brief]
- [3]. Attia SM. Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells. Journal of applied toxicology : JAT. 2013 Jun;33(6):426-33. [Content Brief]
- [4]. Kao-Shan CS, et al. Cytogenetic effects of amsacrine on human lymphocytes in vivo and in vitro. Cancer treatment reports. 1984;68(7-8):989-97. [Content Brief]
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