- ABT 492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms. in vitro:
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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Topoisomerase inhibitor
Voreloxin Hcl is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II. -
topoisomerase II IV inhibitor
Levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. -
DNA gyrase and topoisomerase IV inhibitor
Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. -
topoisomerase IV inhibitor
Ciprofloxacin hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, an fluoroquinolone antibiotic that is widely used as an antimicrobial and immunomodulatory agent -
Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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topoisomerase II inhibitor
Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells. -
topoisomerase IIα inhibitor
Dexrazoxane is an intracellular iron chelator and an inhibitor of topoisomerase IIα. -
Topoisomerase I inhibitor
Belotecan, also known as CKD-602, is the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. -
topoisomerase II inhibitor
Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors. - Gemifloxacin Mesylate is a third generation antibacterial quinolone agent that is also fluorinated.
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DNA Topoisomerase I inhibitor
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. -
DNA topoisomerase I inhibitor
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively. -
Topoisomerase I inhibitor
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. -
DNA topoisomerase I/II inhibitor
Intoplicine is a DNA topoisomerase I and II inhibitor. -
antibacterial candidate for clinical trials
Zabofloxacin (DW-224a Free base) is a novel fluoronaphthyridone quinolone with a 7-pyrrolidone substituent that is considered a potent antibacterial candidate for clinical trials. - Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.
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topoisomerase II inhibitor
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor. - 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.
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topoisomerase I inhibitor
Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity. -
Topoisomerase I inhibitor
Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM. - Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
- Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) is the deuterium labeled banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
- Banoxantrone D12 (AQ4N D12) is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
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gyrase B inhibitor
VXc-486 is a gyrase B inhibitor, with bactericidal activity. -
DNA topoisomerase I inhibitor
Exatecan Mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research. - Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
- Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
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Topoisomerase inhibitor
Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials. -
topoisomerase II inhibitor
Daunorubicin (Daunomycin; RP 13057; Rubidomycin) is a topoisomerase II inhibitor with potent antineoplastic activities. -
ADCs cytotoxin
PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin. -
DNA gyrase/topoisomerase inhibitor
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. -
Topoisomerase agonist
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). -
Alkaloid
Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties.
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Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
Topoisomerase I Inhibitor
Irinotecan hydrochloride is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound exhibits significant anti-tumor activity, primarily in the treatment of colorectal cancers. Its mechanism involves the stabilization of the enzyme-DNA complex, leading to apoptosis in cancer cells. Irinotecan hydrochloride is widely utilized in cancer research to elucidate cellular response mechanisms and to develop novel therapeutic strategies. -
Topoisomerase IIα Inhibitor
Topoisomerase II-IN-24 is a selective inhibitor of Topoisomerase IIα, exhibiting an IC50 of 41.67 μM. This compound has been shown to effectively inhibit the proliferation of cancer cells while inducing G2/M phase arrest and promoting apoptosis. Topoisomerase II-IN-24 is valuable for research focusing on cancer biology, particularly in the study of colon cancer. -
Topoisomerase I/II Inhibitor
Topoisomerase I/II Inhibitor 8 is a dual-target inhibitor that effectively disrupts the function of both Topoisomerase I and II, leading to DNA damage. This compound activates PARP-1, which in turn stimulates the necroptotic pathway via RIPK1, RIPK3, and MLKL signaling. Exhibiting significant anticancer properties, Topoisomerase I/II Inhibitor 8 induces cell death in cancer cells, presenting a promising approach to overcome drug resistance in cancer therapies.

