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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 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. -
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. -
Topoisomerase Inhibitor
Aclacinomycin A hydrochloride is a potent anthracycline antitumor antibiotic that primarily targets topoisomerase I and II. This compound inhibits nucleic acid synthesis, particularly RNA, and may also affect the 26S protease complex along with ubiquitin-ATP-dependent proteolysis. Due to its mechanisms of action, Aclacinomycin A hydrochloride serves valuable applications in cancer research and the study of cellular processes involving nucleic acids and proteolytic pathways. -
Topoisomerases Inhibitor
Pyrazoloacridine is a potent inhibitor of topoisomerases 1 and 2, functioning as an intercalating agent with notable anti-cancer activity. This compound demonstrates cytotoxicity in K562 myeloid leukemia cells, exhibiting an IC50 of 1.25 μM following a 24-hour treatment. Pyrazoloacridine is primarily utilized in cancer research to explore mechanisms of tumor cell proliferation and resistance. -
Topoisomerase II Inhibitor
Etoposide phosphate disodium is a selective inhibitor of topoisomerase II, acting as a potent anti-cancer agent. This phosphate ester prodrug of etoposide effectively prevents the re-ligation of DNA strands, leading to cell cycle arrest, apoptosis, and autophagy in cancer cells. It is utilized in cancer research for its ability to induce programmed cell death and its therapeutic implications in chemotherapy. -
Topoisomerase II Inhibitor
Daunorubicin citrate is a potent inhibitor of topoisomerase II, exerting significant anti-tumor activity. This cytotoxic agent interferes with DNA and RNA synthesis, leading to reduced cancer cell viability and the induction of apoptosis and necrosis. As an anthracycline antibiotic, daunorubicin citrate is utilized in research related to various cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, and Wilms' tumor, as well as studies on infectious diseases. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 11 is a potent inhibitor of topoisomerase II, exhibiting an IC50 of 2.89 μM. It demonstrates significant antiproliferative activity, achieving 92.46% inhibition in the renal cancer cell line A498 with an IC50 of 3.5 μM. This compound induces cell cycle arrest at the G2/M phase, ultimately leading to inhibited cell proliferation and pro-apoptotic effects, making it an important tool for cancer research. -
Topoisomerase Inhibitor
Cholesteryl hemisuccinate is a topoisomerase inhibitor with notable hepatoprotective and anticancer properties. It effectively mitigates acetaminophen-induced hepatotoxicity by preventing hepatic apoptosis and necrosis. Additionally, cholesteryl hemisuccinate interferes with DNA replication and repair mechanisms by inhibiting DNA polymerase and DNA topoisomerase, ultimately leading to reduced tumor growth. This compound is suitable for applications in cancer research and liver protection studies. -
Topoisomerase II Inhibitor
Etoposide phosphate is a selective inhibitor of topoisomerase II, instrumental in disrupting DNA re-ligation processes. As the phosphate ester proagent of etoposide, it exhibits potent anti-cancer activity by inducing cell cycle arrest, apoptosis, and autophagy in cancer cells. This compound is primarily employed in cancer research to explore mechanisms of action and potential therapeutic strategies in oncology. -
Topoisomerase II Inhibitor
ICRF-193 is a potent inhibitor of DNA Topoisomerase II, disrupting DNA synthesis and inducing apoptosis in cancer cells. This compound exhibits significant anti-cancer and anti-inflammatory activities, making it valuable for research in oncology and inflammation. Additionally, ICRF-193 demonstrates cardioprotective properties against anthracycline-induced toxicity in cardiomyocytes. It is particularly relevant for studies focusing on acute promyelocytic leukemia, as well as broader investigations into cancer, infection, inflammation, and cardiovascular conditions. -
Topoisomerase Inhibitor
Cholesterol hemisuccinate Tris salt is a topoisomerase inhibitor that exhibits hepatoprotective and anticancer properties. This compound effectively mitigates acetaminophen-induced hepatotoxicity and prevents subsequent hepatic apoptosis and necrosis. By inhibiting DNA polymerase and DNA topoisomerase, it disrupts DNA replication and repair processes, ultimately inhibiting cell division and tumor growth. Additionally, this compound is suitable for buffer preparation in various laboratory applications. -
Topoisomerase Inhibitor
Alternariol is a mycotoxin that functions as an inhibitor of topoisomerase I and II. This compound exhibits biological activities such as inducing apoptosis, triggering cell cycle arrest, and suppressing innate immune responses, making it valuable for cancer research. Additionally, Alternariol has shown weak estrogenic and antiandrogen effects, along with genotoxic and mutagenic properties, which are relevant to studies on endocrine disruption and its implications in toxicology. -
DNA Topoisomerase I Inhibitor
Podocarpusflavone A is a selective inhibitor of DNA topoisomerase I, demonstrating notable anti-proliferative effects. It has been shown to induce apoptosis in MCF-7 breast cancer cells, suggesting its potential as an anti-tumor agent. This compound is suitable for research applications focused on cancer biology and the mechanistic exploration of cell growth regulation. -
Topoisomerase Inhibitor
Amonafide L-malate is a topoisomerase II inhibitor that functions as a DNA intercalator. This compound induces apoptotic signaling by disrupting the interaction between topoisomerase II and DNA, leading to inhibited DNA replication and cell proliferation. Amonafide L-malate is utilized in cancer research to study mechanisms of apoptosis and the effects of topoisomerase inhibition on tumor cells. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 7 is a selective inhibitor of the topoisomerase II alpha subtype, demonstrating an IC50 of 3.19 μM. This compound is capable of inducing cell cycle arrest and apoptosis, making it a valuable tool for research into cancer biology and therapeutic strategies. Its inhibition of topoisomerase II has potential applications in exploring mechanisms of genomic stability and drug resistance in cancer cells. -
Topoisomerase I Inhibitor
Topoisomerase I inhibitor 3 is a potent inhibitor that targets topoisomerase I, interfering with the topoisomerase I-DNA complex. This compound demonstrates significant biological activity by inducing apoptosis in HepG2 cancer cells and causing cell cycle arrest at the G2/M phase. It serves as a valuable tool for research applications related to cancer biology and therapeutic development. -
Topoisomerase I/III Inhibitor
Topoisomerase I/II inhibitor 3 is a dual inhibitor targeting both topoisomerase I and II. This compound exhibits potent anti-proliferative effects, inhibiting cell proliferation, invasion, and migration, while also inducing apoptosis through the PI3K/Akt/mTOR signaling pathway. It is particularly relevant for research applications in liver cancer studies. -
Topoisomerase Inhibitor
Topoisomerase Inhibitor 4 is a potent inhibitor targeting topoisomerase I and II. This compound effectively induces cell cycle arrest in the G2/M phase, leading to apoptosis in various cancer cell lines. Its significant antitumor activity makes it a valuable reagent for cancer research applications focused on exploring mechanisms of cell cycle regulation and apoptosis. -
Topoisomerase II Inhibitor
Topoisomerase IIα-IN-5 is an inhibitor of topoisomerase IIα, effectively interfering with its catalytic activity. It operates by intercalating into DNA and binding to the minor groove, thereby inhibiting the enzyme's function. This compound demonstrates enhanced efficacy and reduced genotoxicity compared to Etoposide, making it a valuable tool for research applications focused on cancer therapy and DNA topology modulation. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-3 is an orally active dual inhibitor targeting topoisomerase and histone deacetylase (HDAC). This compound enhances intracellular levels of reactive oxygen species (ROS), leading to DNA damage and subsequently inhibiting cancer cell colony formation and migration. Additionally, Top/HDAC-IN-3 induces apoptosis and cell cycle arrest in cancer cells. In non-small cell lung cancer (NSCLC) models, it demonstrates significant antitumor activity, achieving a tumor growth inhibition (TGI) of 77.5% at a dosage of 100 mg/kg. -
Topoisomerase I/II Inhibitor
Topoisomerase I/II Inhibitor 4 is a potent dual inhibitor targeting both topoisomerase I and II. This compound exhibits significant anti-proliferative effects, inhibiting cell growth, invasion, and migration while promoting apoptosis in cancer cells. Its primary research applications include studies focused on liver cancer therapeutics and the exploration of topoisomerase-related mechanisms in cellular processes. -
HDAC/ Topo II α Inhibitor
KT32 is a potent dual inhibitor targeting histone deacetylases (HDAC) and topoisomerase II alpha (Topo II α). This compound promotes cell death through the activation of apoptotic pathways, making it valuable for research in cancer biology and therapeutic studies. KT32's ability to modulate chromatin structure and DNA topology renders it an essential tool for exploring the mechanisms of tumor progression and treatment resistance. -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 15 is a selective inhibitor of topoisomerase II, an enzyme critical for DNA replication and repair. This compound induces apoptosis and exhibits potent activity against head and neck tumors, making it a valuable tool for cancer research. Its mechanism of action further highlights its potential in studying the roles of topoisomerases in tumor biology and therapeutics. -
Topoisomerase II Inhibitor
ICRF-196 is a racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193, functioning as a potent inhibitor of DNA Topoisomerase II. This compound effectively inhibits DNA synthesis and promotes apoptosis, exhibiting significant anti-cancer and anti-inflammatory properties. Additionally, ICRF-196 demonstrates cardioprotective effects against anthracycline-induced toxicity in cardiomyocytes. It is applicable in research focusing on cancer, infectious diseases, inflammation, and cardiovascular disorders, including acute promyelocytic leukemia. -
Topoisomerase IV Inhibitor
Ciprofloxacin lactate functions as a potent inhibitor of topoisomerase IV. It is known to induce damage to both mitochondrial and nuclear DNA, resulting in mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Additionally, ciprofloxacin lactate displays significant anti-proliferative properties and promotes apoptosis, making it valuable for various research applications in microbiology and cancer studies. This fluoroquinolone antibiotic also demonstrates strong antibacterial activity, contributing to its utility in infectious disease research. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-1 is a potent dual inhibitor targeting Topoisomerase II (Topo II) and histone deacetylases (HDACs). This compound is known to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit these targets can provide insights into novel cancer treatment strategies. -
Topoisomerase Inhibitor
Topoisomerase I inhibitor 5 is a potent inhibitor that targets topoisomerase I, exhibiting an IC50 value indicative of its efficacy. This compound disrupts DNA processing and significantly inhibits topoisomerase I activity, leading to cell cycle arrest at the G1 phase and inducing apoptosis in MCF-7 cells. Additionally, Topoisomerase I inhibitor 5 demonstrates potential in reversing P-glycoprotein-mediated resistance to Adriamycin, making it a valuable tool for cancer research. -
DNA Topoisomerase II Inhibitor
Topoisomerase IIα-IN-4 is a non-intercalative ATP-competitive inhibitor targeting human DNA topoisomerase II. With an IC50 of 3.8 μM for TopoIIα and 10.1 μM for TopoIIβ, it effectively induces apoptosis and causes cell cycle arrest in HepG2 cells. Its potent antitumor activity against various human cancer cell lines makes Topoisomerase IIα-IN-4 a valuable reagent for cancer research and therapeutic studies. -
CDK2/Topo I Inhibitor
ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development. -
TopoisomeraseI/II Inhibitor
Erythro-Austrobailignan-6 is a selective inhibitor of DNA topoisomerase I and II, exhibiting anti-cancer properties. This compound induces apoptosis in cancer cells while also promoting the phosphorylation of p38 and JNK signaling pathways. Its ability to interfere with DNA replication makes it a valuable tool for research in cancer biology and therapeutic development. -
Top/HDAC Dual Inhibitor
Top/HDAC-IN-2 is a dual inhibitor targeting topoisomerase and histone deacetylases (HDACs). This compound demonstrates significant antitumor activity and effectively induces apoptosis in cancer cells. Its ability to concurrently interfere with these critical pathways makes it a valuable tool for researchers investigating cancer therapeutics and cell death mechanisms. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-2 is a potent dual inhibitor targeting topoisomerase II (Topo II) and histone deacetylases (HDAC). This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for investigating the mechanisms of tumorigenesis and potential therapeutic interventions. Research applications include studies on cancer biology, drug development, and the modulation of epigenetic regulators. -
DNA Topoisomerase II Inhibitor
DNA Topoisomerase II Inhibitor 1 is a potent inhibitor of DNA topoisomerase II, a crucial enzyme involved in DNA replication and maintenance. This compound exhibits significant anti-proliferative activity by inducing apoptosis and causing cell cycle arrest at the sub-G1 phase. It serves as a valuable tool for research in cancer biology and therapeutic studies targeting cell growth and survival pathways. -
HDAC Inhibitor, Topoisomerase I Inhibitor
WJ35435 is a dual-target HDAC and topoisomerase I inhibitor that exerts anticancer activity by inducing DNA damage and promoting cell cycle arrest at the G1 and G2 phases, ultimately leading to apoptosis. This compound enhances histone H3 acetylation and phosphorylation, along with α-tubulin acetylation and the formation of γ-H2AX, thereby effectively demonstrating its anti-HDAC properties. WJ35435 holds potential for advancing research in cancer therapeutics. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 10 is a potent inhibitor of the topoisomerase II enzyme, exhibiting an IC50 value of 7.45 µM. This compound effectively induces cell cycle arrest in the G2-M phase and promotes apoptosis in HepG-2 cells. Additionally, Topoisomerase II inhibitor 10 demonstrates significant anti-proliferative activity against various cancer cell lines, including HepG-2, MCF-7, and HCT-116, making it a valuable tool for cancer research applications. -
Topoisomerase I Inhibitor
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I, a key enzyme involved in DNA replication and repair. This compound disrupts the enzyme's catalytic activity, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. Topoisomerase I inhibitor 11 is primarily utilized in cancer research, particularly for studying mechanisms of drug resistance and the therapeutic potential of targeting Topoisomerase I in various malignancies. -
Topoisomerase Inhibitor
Hycanthone is a potent topoisomerase inhibitor that functions as a thioxanthenone DNA intercalator. It effectively inhibits RNA synthesis and the activity of DNA topoisomerases I and II, leading to a reduction in nucleic acid biosynthesis. Additionally, Hycanthone demonstrates significant inhibition of apurinic endonuclease-1 (APE1) through direct protein binding, with a binding affinity (KD) of 10 nM. This compound is recognized as a bioactive metabolite of Lucanthone and is noted for its anti-schistosomal properties, making it valuable in related research applications. -
Topoisomerase Inhibitor
Netropsin dihydrochloride is a potent topoisomerase inhibitor that functions as a minor-groove binder. It effectively inhibits the catalytic activity of isolated topoisomerases, disrupting the stabilization of cleavable complexes associated with topoisomerase I and II in the nucleus. Additionally, netropsin dihydrochloride exhibits notable antibacterial and antiviral properties, making it valuable for various research applications, including studies on DNA topology and therapeutic interventions against microbial infections. -
Topoisomerase II Inhibitor
F-14512 is a topoisomerase II inhibitor that selectively targets cancer cells via the polyamine transport system. By enhancing the interaction of polyamines with DNA, F-14512 effectively inhibits topoisomerase II, leading to significant DNA damage and subsequent cellular cytotoxicity, particularly in cells exhibiting high PTS activity. This compound has demonstrated potent antitumor efficacy in the MX1 breast tumor xenograft model, making it a valuable tool for researching breast cancer and exploring mechanisms of drug resistance in oncological studies. -
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. -
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. -
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.

