Catalog No.
Product Name
Application
Product Information
Citations
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Topoisomerase I Inhibitor
Topoisomerase I inhibitor 7 is a potent inhibitor of the enzyme topoisomerase I, demonstrating significant antitumor activity. This compound has shown to inhibit tumor growth by up to 79% and enhance the lifespan of P388 lymphoma-bearing mice by 153%. Its structure suggests promising avenues for the development of new antitumor agents derived from heteroarene-fused anthraquinones, making it a valuable tool for cancer research. -
Camptothecin Analog
TLC388 is a novel camptothecin analog targeting topoisomerase I, exhibiting potential antitumor activity in metastatic neuroendocrine carcinoma (NEC). Its unique chemical structure enhances its efficacy in disrupting DNA replication and transcription processes. This compound is valuable for research applications focused on understanding camptothecin derivatives in cancer therapy and exploring mechanisms of drug resistance in NECs. -
Topoisomerase I/II Inhibitor
Topoisomerase I/II Inhibitor 7 is a potent inhibitor targeting both topoisomerase I and II enzymes. This compound disrupts the enzymatic activity essential for DNA replication and repair, making it a valuable tool for studying mechanisms of cancer cell proliferation and drug resistance. Its applications extend to cancer research, where it can aid in the development of therapeutic strategies targeting topoisomerase activity. -
Topoisomerase I Inhibitor
Chimmitecan, a potent topoisomerase I inhibitor, represents a novel 9-small-alkyl-substituted lipophilic camptothecin derivative. This compound demonstrates significant anticancer activity, making it valuable for research focused on cancer therapies and mechanisms of drug resistance. Its ability to interfere with DNA topology positions Chimmitecan as a key tool in the study of tumor biology and the development of targeted cancer treatments. -
Topoisomerase Inhibitor
(R)-Amrubicin is a topoisomerase II inhibitor and an anthracycline derivative that intercalates into DNA, effectively disrupting DNA replication and impeding RNA and protein synthesis. This results in significant inhibition of cell growth and induction of apoptosis, making it a promising candidate for lung cancer treatment. Notably, (R)-Amrubicin demonstrates enhanced anti-tumor efficacy relative to traditional anthracyclines and exhibits a reduced risk of cumulative cardiac toxicity, providing a safer alternative for cancer therapy. -
Topoisomerase Inhibitor
NBTIs-IN-6 is a potent bacterial topoisomerase inhibitor that exhibits significant antibacterial activity. Notably, it demonstrates an MIC90 of 2 μg/mL against fluoroquinolone-resistant Methicillin-resistant Staphylococcus aureus (MRSA). This compound is valuable for research applications aimed at understanding bacterial resistance mechanisms and developing new antimicrobial therapies. -
Topo II Inhibitor
Topoisomerase II inhibitor 12 is a selective inhibitor of topoisomerase II, functioning as a DNA non-intercalator. It exhibits significant antineoplastic activity, making it a valuable reagent in cancer research. This compound is suitable for studies focused on elucidating the mechanisms of action of topoisomerase II inhibitors and their therapeutic potential in oncology. -
Human DNA topoisomerase II Inhibito
MSN8C is a novel catalytic inhibitor of human DNA topoisomerase II. This compound induces apoptosis in cancer cells and demonstrates significant anti-tumor activity in vitro. MSN8C can be utilized in research applications focused on cancer biology and therapeutic development targeting topoisomerase II pathways. -
DNA Topoisomerase I/II Inhibitor
Corydamine is a 3-arylisoquinoline alkaloid that serves as a potent inhibitor of DNA topoisomerase I and II. This compound exhibits significant anti-cancer activity and is utilized in research applications aimed at understanding the mechanisms of tumorigenesis and the development of targeted cancer therapies. Its ability to interfere with DNA manipulation makes it an important tool in the study of cellular processes and treatment modalities in oncology. -
Topoisomerase I Inhibitor
Topoisomerase I Inhibitor 4 is a selective inhibitor of topoisomerase I, effectively targeting the enzyme to disrupt DNA replication. It demonstrates significant anti-proliferative effects on various cancer cell lines, including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. This compound is valuable for cancer research, particularly in studying mechanisms of tumor growth inhibition. -
Topoisomerase II Inhibitor
Pericosine A is a potent inhibitor of topoisomerase II, derived from the Periconia byssoides strain. This compound exhibits significant antitumor activity, demonstrating efficacy in both in vitro and in vivo settings, making it a valuable tool in cancer research. Additionally, Pericosine A inhibits the epidermal growth factor receptor (EGFR) kinase, further expanding its potential applications in therapeutic research targeting malignancies. -
Topoisomerase-1 Inhibitor
TP3011 (CH0793011) is a potent topoisomerase I inhibitor, demonstrating equipotent activity comparable to SN38. It effectively inhibits the growth of various cancer cell lines, exhibiting IC50 values in the sub-nanomolar range in vitro. This compound is valuable for research applications focused on cancer therapy and the study of topoisomerase-targeted mechanisms. -
Topoisomerase Inhibitor
Topoisomerase Inhibitor 2 (18C) is a potent bacterial topoisomerase inhibitor, demonstrating broad-spectrum activity against multidrug-resistant Gram-negative bacteria. This reagent is valuable for research targeting bacterial DNA replication and repair pathways, making it relevant for studies focused on antibiotic resistance mechanisms and the development of novel antimicrobial agents. -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 8 is a potent inhibitor of topoisomerase II, demonstrating an IC50 of 0.52 μM. This compound exhibits significant anti-proliferative activity, effectively arresting the cell cycle at the G2/M phase. It is suitable for research applications involving cancer cell growth and the study of cell cycle regulation. -
Drug Derivative
(Rac)-7-Ethyl-10-hydroxycamptothecin is a derivative of (±)-10-hydroxycamptothecin, an indole alkaloid known for its ability to inhibit topoisomerase I. This compound demonstrates significant anticancer activity across various cancer cell lines, making it a valuable tool for biological research. Its application extends to studying the mechanisms of cancer cell proliferation and the development of novel chemotherapeutic agents. -
Resolvase Inhibitor
A20832 is a selective inhibitor of resolvase, targeting its recombination and topoisomerase activities. This compound effectively disrupts the site-specific recombination mediated by the Tn3-encoded resolvase protein, specifically at the strand cleavage step, while leaving the synapsis process unaffected. A20832 serves as a valuable tool for researchers investigating the mechanisms of genetic recombination and the role of resolvase in various biological contexts. -
Topoisomerase II Inhibitor
Suptopin-2 is a potent inhibitor of topoisomerase II, a key enzyme involved in DNA replication and cell division. By inhibiting this target, Suptopin-2 disrupts cell cycle progression and destabilizes microtubules, leading to cell cycle arrest. This compound plays a crucial role in research focused on cancer biology and the mechanistic study of cellular processes involving nucleocytoplasmic transport, specifically through the regulation of cyclin B1. -
TopoII Inhibitor
Dichlorogelignate is a selective inhibitor of topoisomerase II (Topo II), demonstrating complete inhibition at a concentration of 50 μM. This compound is instrumental in studying the role of Topo II in DNA manipulation processes, making it valuable for cancer research and drug discovery applications targeting cellular proliferation and genomic stability. -
Topoisomerase I Inhibitor
Lurtotecan dihydrochloride is a semisynthetic analog of Camptothecin that acts as a topoisomerase I inhibitor. This compound exhibits significant anticancer activity, making it a valuable tool in cancer research. Its ability to interfere with DNA replication and transcription provides insights into tumor biology and therapeutic strategies. Researchers may utilize Lurtotecan dihydrochloride in studies of cancer cell survival, resistance mechanisms, and drug efficacy. -
Topoisomerase II Inhibitor
Bakuchicin, a topoisomerase II inhibitor derived from Psoralea corylifolia, demonstrates significant biological activity by inhibiting the enzyme's function. In cellular models infected with Simian virus 40 (SV40), Bakuchicin exhibits an IC50 value of 404 μM against topoisomerase II. This compound is primarily utilized in research focused on virology and anti-infection studies. -
Topoisomerase II Inhibitor
Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that serves as a moderate inhibitor of DNA topoisomerase II, with an IC50 value of 571 μM. This compound demonstrates notable cell growth inhibition, exhibiting IC50 values of 117 μM in K562 cells and 218 μM in CHO cells. Topoisomerase IIα-IN-9 is valuable for research applications focused on cancer biology and the mechanisms of drug resistance. -
topoisomerases I/II inhibitor
Becatecarin is an analog of rebeccamycin that primarily targets topoisomerases I and II. This compound exerts antitumor effects by intercalating into DNA, consequently inhibiting the catalytic activity of these enzymes. Due to its mechanism of action, Becatecarin is valuable in cancer research, particularly in studies exploring DNA damage and repair pathways. -
Topoisomerase II Inhibitor
8-Chloro-ATP tetrasodium is an analog of ATP that functions as an inhibitor of topoisomerase II (Topo II). It effectively inhibits DNA synthesis and promotes the formation of DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium also obstructs the ATP hydrolysis activity catalyzed by Topo II. This compound is valuable for research applications focused on cell division, DNA repair mechanisms, and topoisomerase function. -
Weak Inhibitor of Cell Proliferation
(S)-Gyramide A is a weak inhibitor of cell proliferation that targets DNA gyrase. Its primary biological activity involves interference with DNA supercoiling, which can disrupt bacterial cell division. Research applications of (S)-Gyramide A include studies on bacterial growth inhibition and the elucidation of the role of DNA gyrase in cell cycle regulation. This reagent is valuable for investigating potential antibacterial strategies and understanding the molecular mechanisms of cell proliferation. -
Makaluvamines
Makaluvamine A is a naturally occurring compound that targets topoisomerase II, exerting significant inhibitory effects on this enzyme. Derived from Fijian sponges of the genus Zyzzya, Makaluvamine A demonstrates notable cytotoxic activity against HCT-116 human colon cancer cells. This compound may serve as a valuable tool for cancer research and drug development investigations focused on topoisomerase-targeting therapies. -
Anticancer Agent
Ethonafide is an anthracene-derived compound that functions as an anticancer agent by inhibiting topoisomerase II activity. It stabilizes the enzyme-DNA complex, thereby impacting both topoisomerase IIα and β. This mechanism of action makes Ethonafide a valuable tool for research in cancer therapy and the exploration of potential treatments for malignancies. -
Topoisomerase II Inhibitor
HU 331 is a selective inhibitor of Topoisomerase II, demonstrating significant anticancer properties. This compound has exhibited potent inhibitory effects on various human cancer cell lines in vitro, as well as efficacy in reducing the growth of human tumor xenografts in vivo using nude mice models. HU 331 is valuable for research applications focused on cancer biology and therapeutics targeting DNA topology. -
Topoisomerase II Inhibitor
Retelliptine is a Topoisomerase II inhibitor with notable anticancer properties. This derivative of ellipticine demonstrates the ability to bind to DNA, thereby impeding the function of Topoisomerase II during DNA replication. Its mechanism of action makes it valuable in the study of cancer therapeutics and cell cycle regulation. -
SN-38 Derivative
10-Boc-SN-38 is a tert-butyloxycarbonyl (Boc)-protected derivative of SN-38, the active metabolite of the chemotherapeutic agent Irinotecan. This compound serves as a valuable tool in the study of anti-cancer mechanisms and drug metabolism. Its modification allows for enhanced stability and selectivity in various biological assays, making it useful for drug development and pharmacological research applications. -
Topoisomerase I inhibitor
Topoisomerase I inhibitor 9 is a selective inhibitor of leishmanial topoisomerase IB, demonstrating significant antileishmanial activity against Leishmania donovani promastigotes. The compound exhibits an IC50 value of 34.81 μM, indicating its potential utility in research aimed at developing therapeutic strategies for leishmaniasis. This reagent is valuable for studies focusing on the role of topoisomerases in parasite biology and drug discovery efforts targeting leishmaniasis. -
Topo II Catalytic Inhibitor
NU/ICRF 500 is a potent inhibitor of topoisomerase II catalytic activity, critical for DNA replication and repair. This compound has been shown to increase the formation of CREST-negative micronuclei in human lymphocytes, highlighting its role in genotoxicity studies and cancer research. It serves as a valuable tool for investigating the mechanisms of DNA damage and the effects of topoisomerase inhibition in various biological contexts. -
Top1 Catalytic Inhibitor
Guajadial C is a potent Topoisomerase I (Top1) catalytic inhibitor that effectively delays the DNA damage typically induced by Top1 poisons. This compound exhibits significant cytotoxicity towards various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic strategies targeting Top1-mediated pathways. Its potential applications include investigations into mechanisms of resistance and the development of novel anticancer therapies. -
Topo II Inhibitor
9-Hydroxyellipticin is a potent inhibitor of topoisomerase II (Topo II) and ryanodine receptors (RyR), demonstrating high affinity for DNA with a pKa value of 9.8 at pH 7.4. This compound exhibits significant antitumor and antioxidant activities, with IC50 values of 1.6 μM in HeLa S-3 cells and 1.2 μM in 293T cells. Additionally, 9-hydroxyellipticin has shown promising anticancer effects in murine models of L1210 leukemia, making it a valuable reagent for cancer research and therapeutic studies. -
DNA topoisomerase Inhibitor
Tafluposide is a potent DNA topoisomerase inhibitor that exhibits significant antitumor activity. This compound interferes with DNA replication and transcription processes, making it a valuable tool for cancer research. Its ability to disrupt the normal workings of topoisomerases positions tafluposide as a promising candidate for further studies in cancer therapy. -
Topoisomerases II Inhibitor
8-Chloro-ATP is an analog of ATP that serves as a potent inhibitor of topoisomerase II (Topo II). This compound effectively inhibits DNA synthesis and induces the formation of DNA double-stranded breaks (DSBs) through its action on Topo II-catalyzed ATP hydrolysis. It is a valuable tool for research applications focused on understanding the mechanisms of DNA replication and the role of topoisomerases in cellular processes. -
Intermediate Reactant
(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate serves as an intermediate reactant in the synthesis of Camptothecin, a potent inhibitor of DNA topoisomerase I. With an IC50 value of 679 nM, Camptothecin exhibits significant biological activity in cancer research, particularly in targeting cell division and apoptosis. This compound is essential for studies focused on the development of antitumor agents and the exploration of related therapeutic applications. -
Topoisomerase 1 Inhibitor
VIP236 is a potent topoisomerase 1 inhibitor that selectively targets αvβ3 integrin for tumor localization. Upon binding, VIP236 leverages its cleavable linker, which is activated by neutrophil elastase prevalent in the tumor microenvironment, to deliver 7-ethylcamptothecin directly to cancer cells. This payload induces DNA damage through topoisomerase 1 inhibition, resulting in significant anti-tumor effects. VIP236 has demonstrated a 10-fold increased tumor/plasma ratio compared to traditional treatments, inducing tumor regression and reducing metastasis in various preclinical models, including non-small cell lung cancer, triple-negative breast cancer, and other metastatic solid tumors. -
DNA Topoisomerase IV Inhibitor
Topoisomerase IV inhibitor 1 is a selective inhibitor of DNA topoisomerase IV, exhibiting an IC50 value of 0.23 μM, which highlights its potent activity. It additionally demonstrates inhibitory effects on DNA gyrase with an IC50 of 0.43 μM. This compound showcases significant antibacterial properties, with minimum inhibitory concentrations (MICs) of 0.972 μM against Staphylococcus aureus Newman and 0.608 μM against Escherichia coli ATCC8739. It is ideal for research applications focused on bacterial topoisomerase mechanisms and the development of novel antimicrobial agents. -
Bacterial Topoisomerase Inhibitor
Topoisomerase Inhibitor 5 is a potent bacterial topoisomerase inhibitor, exhibiting a low inhibitory concentration of 0.125 µg/mL. This compound demonstrates significant antituberculous activity, making it valuable for the study of tuberculosis and related bacterial infections. Its mechanism of action primarily involves the disruption of DNA topology, which is essential for bacterial replication and survival. -
DNA Topoisomerase IV Inhibitor
Topoisomerase IV inhibitor 2 is a potent inhibitor of DNA topoisomerase IV, exhibiting IC50 values of 0.35 μM and 0.55 μM against topoisomerase IV and DNA gyrase, respectively. This compound demonstrates significant anti-bacterial activity, with minimum inhibitory concentrations (MICs) of 1.985 μM against Staphylococcus aureus Newman and 0.744 μM against Escherichia coli ATCC8739. It serves as a valuable tool for investigating bacterial topoisomerases and exploring novel antibacterial strategies in research applications. -
Topoisomerase II Inhibitor
TP0480066 is a selective inhibitor of topoisomerase II, demonstrating IC50 values of 1.10 nM and 62.89 nM for DNA gyrase and topoisomerase IV, respectively. This compound exhibits significant antibacterial activity against various bacterial species, including drug-resistant strains. Additionally, TP0480066 shows potent inhibitory effects against Neisseria gonorrhoeae, making it a valuable reagent for research focused on gonorrhea and related bacterial infections. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 16 (compound CT3) is an irreversible inhibitor that selectively targets trypanosomal topoisomerase II by stabilizing double-stranded DNA-enzyme cleavage complexes. This compound demonstrates significant brain penetration and exhibits oral bioavailability, making it a valuable tool for research focused on Chagas disease and related trypanosomal infections. Its distinct mechanism of action underscores its potential utility in exploring therapeutic strategies against these diseases. -
Topoisomerase II Inhibitor
Anti-Trypanosoma cruzi agent-9 is a potent inhibitor of topoisomerase II, effectively disrupting DNA replication and cellular division in target organisms. This compound exhibits significant biological activity against Trypanosoma cruzi, the causative agent of Chagas disease, as well as Leishmania donovani, which is responsible for leishmaniasis. It is a valuable tool for research applications aimed at understanding the mechanisms of these parasitic infections and developing novel therapeutic strategies. -
DNA Gyrase/Topoisomerase IV Inhibitor
Topoisomerase Inhibitor 6 is a dual irreversible inhibitor targeting DNA gyrase and topoisomerase IV, demonstrating a minimum inhibitory concentration (MIC) of 0.06 μg/mL against fluoroquinolone-resistant Staphylococcus aureus. This compound functions by obstructing the DNA strand break-reunion process, thereby causing lethal DNA damage. It holds potential for the study of Gram-positive bacterial infections, including those caused by S. aureus and Streptococcus pneumoniae. -
Topoisomerase II Inhibitor
NBTI 5463 is an inhibitor of bacterial type II topoisomerases, specifically targeting topoisomerase II. This compound exhibits potent antibacterial activity by inhibiting GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. By binding to topoisomerase II, NBTI 5463 disrupts DNA cleavage and religation, thereby obstructing bacterial DNA replication and transcription. This compound holds promise for advancing research on Gram-negative bacterial infections. -
Topoisomerase II Inhibitor
(-)-BO 2367 is a potent topoisomerase II inhibitor, exhibiting significant antibacterial and antitumor properties. It demonstrates IC50 values of 3.8 μM against the DNA relaxation activity of L1210 topoisomerase II and 0.5 μM and 1 μM against the supercoiling activities of Escherichia coli and Micrococcus luteus gyrases, respectively. This compound is valuable for research applications in cancer biology and microbial resistance studies, facilitating further exploration of therapeutic interventions. -
Topoisomerase Inhibitor
(±)-10-Hydroxycamptothecin is a potent topoisomerase I inhibitor known for its significant anticancer properties. This indole alkaloid demonstrates a broad spectrum of biological activity, making it a valuable reagent in cancer research. Its ability to interfere with DNA replication makes it a critical compound for studies focused on targeted therapies and drug resistance mechanisms in cancer cells. -
Topoisomerase II Inhibitor
Pixantrone is a potent topoisomerase II inhibitor and DNA intercalator, demonstrating significant anti-tumor activity. This compound interferes with DNA replication and transcription processes, making it valuable for cancer research. Its application spans various oncology studies, particularly in evaluating therapeutic effects against different tumor types.
