Exatecan TFA, a methylpropanamide-modified derivative of the common ADC cytotoxin Exatecan, serves as a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM (0.975 μg/mL), utilized in the synthesis of ADCs for cancer research [1].

AuM1Phe, an N-heterocyclic carbene (NHC) metal complex, inhibits both human topoisomerase I activity and actin polymerization. It also impedes the proliferation of MDA-MB-231 breast cancer cells, exhibiting an IC50 value of 1.2 μM [1].

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin. Doxorubicin is a DNA topoisomerase II inhibitor.

IndiMitecan (LMP776) is an inhibitor of topoisomerase I (Top1) with anticancer activities [1].