Topoisomerase I/II-IN-1 

Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer^[1].

Topoisomerase I/II-IN-1 (Compound 5j) (10 μM) showed inhibitory effects on a variety of cancer cells: the growth inhibition rate (GI) of melanoma LOX IMVI cells was -93.46%, the GI of colorectal cancer HCT-116, HCT-15 and SW-620 cells were -59.51%, -40.12% and -43.01%, respectively, the GI of breast cancer MDA-MB-468 cells was -24.45%, and the GI of renal cancer cells 786-0, RXF 393 and UO-31 cells were -11.21%, -12.44% and -29.74%, respectively^[1].

Topoisomerase I/II-IN-1 inhibits Topo I/Topo IIβ enzyme activity by 61.58%/75.51% in LOX IMVI cell lines and 56.42%/76.39% in HCT-116 colon cancer cells, respectively^[1].

Topoisomerase I/II-IN-1 (24 hours) induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, cleaved caspase-3 protein levels, and the Bax/Bcl-2 ratio, and downregulating Bcl-2 in HCT-116 and LOX IMVI cells^[1].

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

614.62

C₃₃H₃₁FN₄O₇

O=C(C1CC=C(C(CN2CCN(CC2)C3=C(C=C4C(C(C(O)=O)=CN(C4=C3)C5CC5)=O)F)=C1)O)/C=C/C6=CC=CC([N+]([O-])=O)=C6

Room temperature in continental US; may vary elsewhere.

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

• [1]. Abdel-Rahman IM, et al.Unveiling ortho-phenolic Mannich ciprofloxacin-chalcone conjugates with potential antineoplastic activity: synthesis, mechanistic study, in silico docking and molecular dynamic simulation. Eur J Med Chem. 2025 Oct 15;296:117891.  [Content Brief]