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Catalog No.
Product Name
Application
Product Information
Citations
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DNA gyrase/topoisomerase inhibitor
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. -
topoisomerase II inhibitor
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor. -
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. -
gyrase B inhibitor
VXc-486 is a gyrase B inhibitor, with bactericidal activity. -
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. -
Topoisomerase I Inhibitor
Topoisomerase I Inhibitor 2 targets DNA topoisomerase I (Top1) with high specificity, effectively inhibiting its activity and leading to DNA damage. This compound not only induces apoptosis but also disrupts the G2/M phase of the cell cycle, thereby exhibiting significant anti-tumor effects. Its properties make it a valuable tool for cancer research and therapeutic studies focused on DNA damage response mechanisms. -
HDAC/Top Inhibitor
HDAC/Top-IN-1 is a potent dual inhibitor targeting histone deacetylases (HDACs) and topoisomerases, with IC50 values of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM, and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. This compound effectively induces apoptosis and S phase cell-cycle arrest in HEL cells, demonstrating its antiproliferative properties. Additionally, HDAC/Top-IN-1 exhibits significant in vivo antitumor efficacy, making it a valuable tool for cancer research applications. -
DNA Topoisomerase I Inhibitor
Isodiospyrin is a natural dimeric naphthoquinone that functions as an inhibitor of human DNA topoisomerase I. By blocking DNA relaxation and the kinase activities of this enzyme, Isodiospyrin exhibits significant anticancer, antibacterial, and antifungal properties. This compound is valuable for research applications focused on cancer therapy and microbial resistance. -
DNA Topoisomerase II/Topoisomerase I Inhibitor
Eupolauridine is a selective inhibitor of DNA topoisomerase II, showing inhibitory concentrations (IC50) of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. This compound exerts antifungal activity by impairing the catalytic function of topoisomerase II and stabilizing its cleavage complex with DNA, resulting in DNA damage. Eupolauridine holds potential for research applications in the study of fungal infectious diseases. -
Topoisomerase I/II Inhibitor
Luotonin A is a potent inhibitor of topoisomerase I and II. It exhibits significant antiviral activity against tobacco mosaic virus (TMV) and demonstrates antitumor properties. This compound is valuable for research applications in virology and oncology, providing insights into enzyme inhibition and potential therapeutic strategies against viral infections and cancer. -
Topoisomerase I/II Inhibitor
SelB-1 is a dual inhibitor targeting Topoisomerase I and II, demonstrating significant anticancer activity. This compound is particularly useful in the study of prostate and colon cancers. Additionally, SelB-1 induces autophagy gene expression and lipid peroxidation, while effectively lowering glutathione (GSH) levels, providing insights into its mechanistic roles in cancer biology. -
Topoisomerase I Inhibitor
Irinotecan-d10 is a deuterated derivative of Irinotecan, a potent inhibitor of topoisomerase I. By binding to the topoisomerase I-DNA complex, it disrupts the religation of DNA strands, thereby inducing DNA damage and apoptosis in rapidly dividing cells. This reagent is useful in cancer research, particularly in studies aimed at understanding the mechanisms of action of topoisomerase inhibitors and their therapeutic potential in oncology. -
DNA Gyrase/Topoisomerase Inhibitor
Levofloxacin sodium is a potent DNA gyrase and topoisomerase IV inhibitor that exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. Its primary applications include research on chronic periodontitis, airway inflammation, and BK viremia. Additionally, Levofloxacin sodium demonstrates anti-orthopoxvirus properties, making it a valuable reagent for studies involving viral infections. -
Topoisomerase I Inhibitor.
T-2513 hydrochloride is a selective inhibitor of topoisomerase I. By covalently binding to and stabilizing the topoisomerase I-DNA complex, it effectively inhibits DNA replication and RNA synthesis, resulting in cytotoxicity. This compound is utilized in research applications focused on cancer biology and the mechanisms of chemotherapeutic agents. -
Topoisomerase II Inhibitor
NK-611 is a topoisomerase II inhibitor that functions as an epipodophyllotoxin derivative. By inhibiting topoisomerase II with an IC50 of 56 μM, NK-611 induces DNA double-strand breaks, leading to effective antitumor activity. Unlike its parent compound Podofilox, NK-611 does not interfere with microtubule polymerization, thus minimizing associated side effects. This compound has shown potent efficacy in in vivo leukemia models and is valuable for cancer research applications. -
Topoisomerase I Inhibitor
T-2513 is a selective inhibitor of topoisomerase I, a critical enzyme involved in the relaxation of DNA supercoils during replication and transcription. By covalently binding to and stabilizing the topoisomerase I-DNA complex, T-2513 effectively inhibits DNA replication and RNA synthesis. This activity may induce cytotoxic effects, making it a valuable tool in cancer research and studies focused on cell proliferation and death. -
Topoisomerase II Inhibitor
F-14512 hydrochloride is a potent inhibitor of topoisomerase II, functioning through the polyamine transport system (PTS) to selectively target cancer cells. By enhancing the binding affinity of polyamines to DNA, it effectively inhibits topoisomerase II activity, leading to significant cytotoxic effects in cells with elevated PTS activity and resulting in DNA damage. Additionally, F-14512 hydrochloride exhibits strong antitumor efficacy in the MX1 breast tumor xenograft model, making it a valuable reagent for cancer research, particularly in studies focusing on breast cancer. -
DNA topoisomerase II Inhibitor
NSC 660028 is a potent inhibitor of DNA topoisomerase II, exhibiting an ID50 of 50 μM. This compound disrupts DNA topoisomerase II activity, leading to the induction of protein-linked DNA breaks. NSC 660028 is primarily utilized in cancer research to explore mechanisms of tumor cell proliferation and resistance. -
Topoisomerase II Inhibitor
KW-2170 hydrochloride is a potent topoisomerase II inhibitor that functions by stabilizing the topoisomerase II-DNA complex. This stabilization leads to DNA double-strand breaks, thereby inhibiting DNA replication and transcription, which ultimately results in tumor cell death. KW-2170 hydrochloride demonstrates broad-spectrum anti-tumor activity in various mouse and human tumor models, making it a valuable reagent for research related to solid tumors. -
Topoisomerase Inhibitor
NSC 727357 is a potent topoisomerase inhibitor and DNA intercalator, exhibiting significant antitumor activity. It effectively inhibits cell proliferation and induces G1 phase cell cycle arrest. This compound is particularly relevant for cancer research, including studies focused on melanoma. -
Topoisomerase Inhibitor
Netropsin is a small-molecule minor-groove binder that functions as a topoisomerase inhibitor. It effectively inhibits the catalytic activity of isolated topoisomerase, disrupting the stabilization of cleavable complexes associated with both topoisomerase I and II. Additionally, Netropsin exhibits antibacterial and antiviral properties, making it a valuable tool for research in the fields of microbiology and virology. -
Topoisomerase II/DNA Polymerase Inhibitor
Epolactaene is a potent inhibitor of Topoisomerase II and DNA Polymerases, exhibiting IC50 values of 10 µM for Topoisomerase II, 25 µM for DNA Polymerase α, and 94 µM for DNA Polymerase β. Its ability to interfere with these key enzymes makes Epolactaene valuable for studying DNA replication and repair mechanisms. This compound is suitable for research applications involving cancer biology and the investigation of DNA-targeting therapies. -
Topoisomerase II Inhibitor
Amrubicin hydrochloride is a potent inhibitor of DNA topoisomerase II, a key enzyme involved in DNA replication and repair. This compound exhibits significant antitumor activity and has been studied for its efficacy in various cancer models. It is utilized in research to explore mechanisms of action in chemotherapy and to evaluate potential therapeutic strategies against tumors. -
TROP2 Directed Agent, Topoisomerase I Inhibitor
Sacituzumab tirumotecan is an antibody-drug conjugate that functions as a TROP2-directed agent and a topoisomerase I inhibitor. With a TROP2 EC50 of 2.787 ng/ml and a topoisomerase I IC50 of 0.7 μmol/L, it effectively delivers its cytotoxic payload to target cells. This compound is utilized in research focusing on metastatic triple-negative breast cancer and metastatic non-small cell lung cancer, making it crucial for studies aimed at understanding treatment mechanisms and therapeutic efficacy in these challenging malignancies. -
Topoisomerase Inhibitor
(4-NH2)-Exatecan is a topoisomerase inhibitor and a derivative of Exatecan. It exhibits significant biological activity by disrupting the DNA replication process, making it a valuable tool in cancer research. Additionally, (4-NH2)-Exatecan is suitable for the synthesis of antibody-drug conjugates (ADCs), facilitating targeted therapeutic applications in oncology. -
Topoisomerase I Inhibitor
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a topoisomerase I inhibitor that effectively interferes with DNA replication and transcription by stabilizing the DNA-enzyme complex. This compound demonstrates significant potential in antibody-drug conjugate (ADC) applications, showing efficient delivery to cells for targeted therapy. Its efficacy has been validated in both in vivo and in vitro models, making it a valuable tool for cancer research and therapeutic development. -
DNA Topoisomerase I Inhibitor
Ac-Exatecan is an acetylation-modified derivative of Exatecan, primarily functioning as an inhibitor of DNA Topoisomerase I, with an IC50 of 2.2 μM. This compound exhibits significant antitumor activity, making it a valuable payload for antibody-drug conjugate (ADC) applications. Ac-Exatecan is particularly effective against cells with P-glycoprotein-mediated multidrug resistance, offering potential in overcoming therapeutic challenges associated with resistant tumor types. -
DNA topoisomerase I Inhibitor
(αR)-Cyclopropaneacetamide-Exatecan is a potent inhibitor of DNA topoisomerase I, exhibiting enhanced membrane permeability with an IC50 value of 1.34 μM against the human enzyme. This compound induces cytotoxicity through the suppression of topoisomerase I activity, displaying anticancer effects that are independent of HER2 expression levels. Derived from Exatecan, (αR)-Cyclopropaneacetamide-Exatecan serves as an antibody-drug conjugate cytotoxin and is applicable in research on various advanced cancers, including breast, gastric, colorectal, and non-small cell lung cancers. -
Topoisomerase Inhibitor
Mal-Exatecan is a maleimide-modified derivative of Exatecan, acting primarily as a DNA topoisomerase I inhibitor. This compound demonstrates potent antitumor activity by stabilizing the topoisomerase-DNA complex, leading to DNA strand breaks and subsequent cell death in rapidly dividing cancer cells. Mal-Exatecan is primarily utilized in cancer research to explore therapeutic strategies targeting topoisomerase I. -
DNA topoisomerase I Inhibitor
DRF-1042 is a potent inhibitor of DNA topoisomerase I, derived from Camptothecin. It demonstrates significant anticancer activity against a diverse range of human cancer cell lines, including those exhibiting multi-drug resistance (MDR). This compound is valuable for research applications focused on cancer therapeutics and the mechanisms of resistance in tumor cells. -
Topoisomerase I Inhibitor
Exatecan mesylate dihydrate is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 of 2.2 μM (0.975 μg/mL). This compound is particularly relevant in cancer research, as it interferes with DNA relaxation during replication, subsequently leading to apoptosis in rapidly dividing cells. Its application extends to various studies focused on chemotherapeutic mechanisms and the development of novel anti-cancer therapies. -
DNA topoisomerase I Inhibitor
Rebeccamycin is a potent inhibitor of DNA topoisomerase I, a key enzyme involved in DNA replication and transcription. This antitumor antibiotic primarily exerts its cytotoxic effects by stabilizing the topoisomerase I-DNA cleavage complex, leading to DNA damage and apoptosis in cancer cells. Rebeccamycin shows minimal activity against protein kinase C and topoisomerase II, making it a selective agent for research in cancer biology and therapeutic development. -
Topoisomerase I Inhibitor
Exatecan hydrochloride is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 value of 2.2 μM (0.975 μg/mL). This compound is primarily utilized in cancer research, facilitating investigations into the mechanisms of tumor cell proliferation and survival by disrupting the topological state of DNA during replication. Its activity makes it a valuable tool for exploring therapeutic options and treatment strategies in oncology. -
Topoisomerase I Inhibitor
Exatecan analog 38 is a potent topoisomerase I inhibitor derived from camptothecin. This compound exhibits significant cytotoxicity against various cancer cell lines, making it a valuable tool for oncology research. Exatecan analog 38 can be utilized in the development of antibody-drug conjugates (ADCs) by conjugating it to monoclonal antibodies through linkers, enhancing targeted therapeutic applications. -
Topoisomerase I Inhibitor
LD2-3 is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound can be conjugated to monoclonal antibodies via linkers to create antibody-drug conjugates (ADCs), facilitating targeted therapy applications. LD2-3 is particularly suited for use in studies involving carcinoembryonic antigen (CEA) overexpressing tumors, enabling researchers to explore its efficacy in a precision oncology context. -
DNA Topoisomerase Inhibitor
(5-Cl)-Exatecan is a potent inhibitor of DNA topoisomerase, primarily utilized in cancer research settings. This compound functions as an antibody-drug conjugate (ADC) cytotoxin, targeting and disrupting the DNA replication process in cancer cells. Its efficacy in selectively inducing cytotoxicity makes it a valuable tool for studying cancer therapeutics and exploring the mechanisms of drug resistance. -
Topoisomerase Inhibitor
MC-DOXHZN (hydrochloride) is a topoisomerase II inhibitor that serves as an albumin-binding proagent of Doxorubicin. This compound features acid-sensitive properties, enabling it to selectively release Doxorubicin in tumor microenvironments. MC-DOXHZN is particularly valuable for antibody-drug conjugate (ADC) synthesis, facilitating targeted cancer therapies. Its unique mechanism enhances the potential for effective treatment strategies in oncology research. -
Topoisomerase II α/β Inhibitor
Chloroquinoxaline sulfonamide is a potent inhibitor of topoisomerase II α/β, disrupting the enzyme's function and causing DNA damage. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Additionally, it is employed in veterinary medicine to control coccidiosis in various livestock, including poultry, rabbits, sheep, and cattle. Its varied applications underscore its importance in both therapeutic and research settings. -
Telomerase Inhibitor
MST-312 is a telomerase inhibitor developed as a chemically modified derivative of epigallocatechin gallate (EGCG) found in green tea. It demonstrates significant biological activity by selectively inhibiting telomerase, an enzyme commonly associated with cancer cell immortality. MST-312 is primarily utilized in cancer research, particularly in the study of multiple myeloma and other malignancies, offering insights into potential therapeutic strategies targeting telomerase activity. -
Telomerase Inhibitor
Telomerase-IN-3 is a potent telomerase inhibitor that directly targets the activity of the hTERT promoter. By inhibiting hTERT, this compound plays a critical role in reducing telomerase activity, thereby impacting cellular lifespan and growth. Telomerase-IN-3 is useful for research applications focused on cancer biology, cellular aging, and the development of therapies aimed at telomerase-related diseases. -
TRF2 Inhibitor
FKB04 is a potent inhibitor of telomeric repeat binding factor 2 (TRF2), impairing telomere maintenance mechanisms in liver cancer cells. This activity results in T-loop defects, telomere shortening, and subsequent cellular senescence. FKB04 has demonstrated efficacy in inhibiting tumor growth in human liver cancer xenograft models, notably in BALB/c mice implanted with Huh-7 cells. Its application is primarily in liver cancer research, making it a valuable tool for exploring therapeutic strategies targeting telomere dynamics. -
Telomerase Inhibitor
Telomerase-IN-1 is a potent telomerase inhibitor, exhibiting an IC50 of 0.19 µM. This compound effectively targets telomerase activity, making it a valuable tool for investigating telomerase-related mechanisms in cellular biology. Its application is particularly relevant in cancer research, where telomerase activity is often upregulated, contributing to unlimited cellular proliferation.
