Topoisomerase IIα-IN-2

Names

[ CAS No. ]:
2407521-90-6

[ Name ]:
Topoisomerase IIα-IN-2

Biological Activity

[Description]:

Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

[Target]

topoisomerase II alpha

topoisomerase II beta


[In Vitro]

Topoisomerase IIα-IN-2 (compound 5) shows antiproliferative activity in cancer cell lines (CCRF-CEM, CCRF-SB, MT-4, HT-29, MCF-7, HeLa, ACHN, SKMEL-28, and G-361), with IC50 values of 0.003, 0.005, 0.006, 0.004, 0.003, 0.005, 0.005, 0.002, and 0.006 μM, respectively[1].

[References]

[1]. Pedatella S, et al. Antitumor agents 7. Synthesis, antiproliferative activity and molecular modeling of new l-lysine-conjugated pyridophenoxazinones as potent DNA-binding ligands and topoisomerase IIα inhibitors. Eur J Med Chem. 2020 Feb 1;187:111960.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20N4O5

[ Molecular Weight ]:
420.42

Related Compounds