Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1[1][2][3][4].
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)[1].
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes[1]. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties[2].
Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner[1][2].
Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively.
SN-38-d5 is deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity[1].
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects[1].
BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity[1].
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[1][2][4][5].
Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase[1].
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR)[1]. Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage[2].
Fmoc-leucine-15N is a 15N-labeled and 13C-labled EIDD-1931. EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine ence
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a drug-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM)[1].
Irinotecan hydrochloride trihydrate is a water soluble topoisomerase I inhibitor with antitumor activity.
Topotecan Hydrochloride (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor with potent antineoplastic activities.
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
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[1].
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect[1].
XR-11576 HCl is a novel orally active dual topoisomerase I and II inhibitor with antitumor activity.
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[1].
PNU-159682, a highly potent metabolite of the anthracycline nemorubicin with outstanding cytotoxicity, is a potent ADCs cytotoxin.
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells[1].
Ungeremine, a phenanthridine type alkaloid, is extracted of the bulbs of Pancratium Illyricum. Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. Ungeremine displays cytotoxic activity towards the 9 cancer cell lines, including drug-sensitive and MDR phenotypes. Ungeremine induced ferroptosis, necroptosis, autophagy as well as apoptosis mediated by caspase activation, MMP alteration and increase ROS production[1][2].
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a drug-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM)[1].
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities[1].
Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells[1].
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[1].
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines[1].