CPT-Se4, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM).

CPT-Se3, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM).

Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.

Sabarubicin is a doxorubicin disaccharide analogue with striking antitumor activity. Sabarubicin is more effective than doxorubicin as a topoisomerase II poison and stimulated DNA fragmentation at lower intracellular concentrations.

CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11).

CP-67015, a nalidixic acid analog, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects.

Diflomotecan (BN 80915) is a potent inhibitor of topoisomerase I. Diflomotecan causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.

Dxd-D5 (Exatecan-D5 derivative for ADC) is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .

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

Huanglongmycin N is a DNA topoisomerase I inhibitor (EC50 = 14 μM).

T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.

Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities.

(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.

Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.

PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).

Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.

Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent.

T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.

Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.

CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).

Exatecan D5 Mesylate (DX8951f-D5) is deuterium labeled Exatecan Mesylate. Exatecan Mesylate is a DNA topoisomerase I, with an IC50 of 0.975 μg/mL.

RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.

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

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

Camptothecin (CPT) is a potent DNA enzyme topoisomerase I (topo I) inhibitor with an IC50 and IC70 of 50 nM and 0.225 μM for breast cancer cell line MDA-MB-231.

Amonafide(AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage.

A doxorubicin analog that demonstrates anti-cancer activity without cardiotoxicity, does not inhibit topoisomerase IIβ activity at 100 uM.