Topoisomerase I-IN-18

Topoisomerase I-IN-18 (Compound 11d) exhibits variable antiproliferative activity across the tested cancer cell lines, including MCF-7 (IC₅₀ = 59.11 μM), HepG-2 (IC₅₀ = 67.63 μM), SGC7901 (IC₅₀ = 44.6 μM), A549 (IC₅₀ = 8.06 μM), and exhibits minimal toxicity towards the normal HK-2 cells^[1].
Topoisomerase I-IN-18 (1-10 μM) effectively blocks Topo I-mediated relaxation of superhelical DNA through dose-dependent inhibition^[1].
Topoisomerase I-IN-18 (1-10 μM, 48 h) elicits dose-dependent DNA double-strand breaks in A549 cells^[1].
Topoisomerase I-IN-18 (1-10 μM, 0-48 h) effectively inhibits A549 cell migration and proliferation, suggesting potential antimetastatic properties^[1].
Topoisomerase I-IN-18 (4-16 μM, 48 h) induces both ROS generation and apoptosis in a dose-dependent manner in A549 cells^[1].
Topoisomerase I-IN-18 (4-16 μM, 24 h) induces dose-dependent S-phase arrest accompanied by reductions in G0/G1 and G2/M populations, and significantly increases γ-H2AX phosphorylation and modulates the expression of key apoptosis-related proteins, evidenced by the upregulation of p53, Bax, caspase-3, and caspase-9 and the downregulation of Bcl-2 in A549 cells^[1].
Topoisomerase I-IN-18 is identified as a P-glycoprotein (P-gp) substrate and a potential inhibitor of cytochrome P450 enzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4)^[1].

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