Topoisomerase I-IN-24

Topoisomerase I-IN-24 (compound 5l) (48 h) potently inhibits the proliferation of A549, HepG2 and HeLa cancer cells, with IC₅₀ values of 5.47 μM, 6.21 μM and 5.53 μM, respectively, while exerting no significant effect on normal LO-2 hepatocytes^[1].
Topoisomerase I-IN-24 (10-100 μM; 30 min) inhibits the activity of human topoisomerase I (Topo I) in a concentration-dependent manner, and completely blocks the relaxation of supercoiled DNA at a concentration of 100 μM^[1].
Topoisomerase I-IN-24 (1.25-5.0 μM; 48 h treatment, followed by 14 days of culture without compound) inhibits the long-term proliferation of A549 cells in a concentration-dependent manner, and its inhibitory effect at 5.0 μM is stronger than that of CPT (HY-16560)^[1].
Topoisomerase I-IN-24 (100 μM; 30 min) is a Topo I poison that stabilizes the Topo I-DNA cleavage complex at a concentration of 100 μM to induce DNA nicks, with a mechanism of action similar to that of CPT^[1].
Topoisomerase I-IN-24 (1.25-5.0 μM; 24 h, 48 h) inhibits the migration of A549 cells in a concentration-dependent manner and reduces the wound healing rate at 24 h and 48 h^[1].
Topoisomerase I-IN-24 (1.25-5.0 μM; 48 h) induces DNA double-strand breaks in A549 cells in a concentration-dependent manner in vitro, and its activity at 5.0 μM is comparable to that of CPT^[1].

Topoisomerase I-IN-24 (1.25-5.0 μM; 24 h) induces apoptosis in A549 cells in a concentration-dependent manner, with a total apoptosis rate of 56.2% at the concentration of 5.0 μM, which is significantly higher than that of CPT^[1].

Topoisomerase I-IN-24 (1.25-5.0 μM; 24 h) induces dose-dependent G1/G0 cell cycle arrest in A549 cells, and increases the proportion of G1-phase cells to 70.23% at a concentration of 5.0 μM^[1].

Topoisomerase I-IN-24 (1.25-5.0 μM; 24 h) induces mitochondrial dysfunction in A549 cells in a concentration-dependent manner in vitro, leading to the loss of mitochondrial membrane potential^[1].

Topoisomerase I-IN-24 (1.25-5.0 μM; 12 h) increases intracellular ROS levels in A549 cells, with significant elevations observed at concentrations of 2.5 μM and 5.0 μM^[1].