Topoisomerase I inhibitor 17

Topoisomerase I inhibitor 17 (5-500 nM, 72 h) is antiproliferative to four cancer cells (HepG2, A549, HeLa and HCT116) with IC₅₀s of 136.6, 33.7, 72.9 and 36.1 nM, respectively^[1].
Topoisomerase I inhibitor 17 is translocated across the Caco-2 cell monolayer with an apparent permeability coefficient of 2.24 μcm/s from apical to basolateral (0.5-1.0 μM, 4 h), with viability of Caco-2 cells greater than 90% (0.2-1.0 μM, 4 h)^[1].
Topoisomerase I inhibitor 17 (5-100 nM, 12-72 h) significantly inhibits proliferation-induced colony formation, concentration-dependently inhibits HCT116 cell migration, and increases ROS generation^[1].
Topoisomerase I inhibitor 17 (0-50 μM, 48 h) induces apoptosis and cell cycle arrest in a dose-dependent manner and blocks the progression of the G2/M checkpoint in HCT116 cells^[1].
Topoisomerase I inhibitor 17 inhibits DDX5 expression in HCT116 cells (100 nM, 48-72 h) and deregulates DDX5-blocked Top1 activity (5 and 50 μM) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.