Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

Cytosine β-D-arabinofuranoside hydrochloride is an anti-leukemic agent which binds to topoisomerase I resulting in DNA fragmentation and inhibition of replication. In addition this compound does not have any effects on RNA synthesis. Cytosine β-D-arabinof

SN-38(NK-012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

LMP744 (MJ-III-65, NSC706744) is a small molecule TOP1 inhibitor antitumoral activity.

Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic and water-soluble camptothecin derivative.

Idarubicin Hcl is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor.

Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II.

Voreloxin(SNS-595; AG 7352) is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II.

SW-044248 is a Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines.

Irinotecan(CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.

Ellipticine hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.

TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea.

Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.

Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.

Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.

Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity.

Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties.

SDOX is the Doxorubicin (DOX) prodrug. The loaded DOX prodrugs (SDOX) which can release the parent drugs DOX triggered by excessive GSH in tumor cells, minimize the unexpected side effects on normal tissues without compromising the potency.

Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.

AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria.

TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

LMP517 (NSC 781517) is a non-camptothecin, dual TOP1 and TOP2 topoisomerase inhibitor.LMP517 showed better antitumor activity than its parent compound LMP744 against H82 (small cell lung cancer) xenografts.

Lapcin is a potent dual topoisomerase I/II inhibitor with nM to pM IC50s against diverse cancer cell lines (Colon cancer HT29 cell IC50=0.516 nM); Lapcin showed weak activity against DNA gyrase (IC50>20.5 uM). While only weakly active against DNA gyrase, lapcin was a potent of inhibitor of both DNA relaxation by topoisomerase I (IC50=2.17 uM) and DNA decatenation by topoisomerase II (IC50=7.53uM), 14 times more potent than the alkaloid camptothecin. Lapcin was more potent than the topoisomerase II inhibitor etoposide against all of the cell lines we tested, with the exception of the lung cancer cell NCI-H226, against which it was essentially equipotent. Cell lines expressing wild-type p53 (HCT116, H226, MCF7) tended to show higher IC50s than p53 reduced cell lines (NCI-H1299, HT29, Colo205, Hela).

HH-N25 is a a potent and selective topoisomerase I (TOP1) inhibitor with potent antiproliferative activities against a panel of human breast cancer cell lines (IC50=0.045-4.2 uM).HH-N25 shows potent antitumor activities in human breast cancer cells in vitro and in vivo.

Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer.