DNA/TOP2A-IN-1

DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Microtubule/Tubulin; Reactive Oxygen Species (ROS) ; Topoisomerase

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

COC1=CC=C(C=C1)OC2=C(C(C)=NN2C)CNC(C3=CC4=C(C(C5=CC=C(C=C5)OC)=N3)NC6=CC=CC=C64)=O

Molecular Formula

C32H29N5O4

Molecular Weight

547.60

References & Citations

[1] Xu X, et al. Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer. Eur J Med Chem. 2025 Nov 15;298:118041.