Topoisomerase I-IN-20 

Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research^[1].

Topoisomerase I-IN-20 (Compound 11d) (25-100 μM; 30 min) inhibits human topoisomerase I-mediated DNA relaxation^[1].
Topoisomerase I-IN-20 potently inhibits the proliferation of human A549 lung cancer cells with an IC₅₀ of 8.06 μM; it exhibits moderate activity against MCF-7, HepG-2 and SGC-7901 cells, and shows extremely low toxicity toward normal HK-2 cells^[1].
Topoisomerase I-IN-20 (0-10 μM; 0-48 h) inhibits migration of human lung adenocarcinoma cell line A549^[1].
Topoisomerase I-IN-20 (4-16 μM; 48 h) increases the intracellular ROS level in human lung cancer A549 cells in a dose-dependent manner^[1].
Topoisomerase I-IN-20 (4-16 μM; 24-48 h) induces S-phase cell cycle arrest and apoptosis in human lung cancer A549 cells^[1].
Topoisomerase I-IN-20 (4-16 μM; 24 h) induces DNA double-strand breaks in human lung cancer A549 cells in a dose-dependent manner (by enhancing γ-H2AX phosphorylation), and activates the mitochondria-mediated apoptotic pathway (by upregulating the expressions of p53, Bax, caspase-3 and caspase-9, while downregulating the expression of Bcl-2)^[1].
Topoisomerase I-IN-20 (1-10 μM; 48 h) induces DNA damage in human lung cancer A549 cells, with significant damage observed at concentrations of 5 and 10 μM^[1].

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

431.61

C₂₃H₃₄FN₅S

NC(N/N=C/CCCC1C2C(N3CCC2)C(CCC3)CN1CC4=CC=C(F)C=C4)=S

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shen G, et al. Design, synthesis, and evaluation of novel matrine derivatives as topoisomerase I inhibitors for anticancer agents. Eur J Med Chem. 2025;300:118082.  [Content Brief]