Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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 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. -
Type IIA Topoisomerases Inhibitor
GSK945237 is a potent inhibitor of bacterial type IIA topoisomerases, exhibiting strong bactericidal activity. It demonstrates broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria, with an IC50 of 0.034 μg/mL against Helicobacter influenzae DNA gyrase. In vivo studies indicate significant effectiveness in a rat model of respiratory tract infection, highlighting its potential applications in anti-infection research. -
Topoisomerase II Inhibitor
CP-67015 is a potent topoisomerase II inhibitor that exhibits direct mutagenic effects in mammalian cells, impacting both gene and chromosomal levels. As a quinolone antibiotic, it demonstrates significant biological activity, making it a valuable tool for researchers investigating DNA manipulation and repair mechanisms. CP-67015 is suitable for studies focused on the role of topoisomerase II in cellular processes and the effects of targeted DNA damage. -
Topoisomerase Inhibitor
(1R,2S,7R)-Sitafloxacin is a potent inhibitor of topoisomerases, specifically targeting DNA gyrase with an IC50 of 0.18 μg/mL. This stereoisomer's activity highlights its potential in elucidating the role of topoisomerase-mediated DNA manipulation in various biological processes. It serves as a valuable tool in molecular and cellular research applications focusing on DNA replication and repair mechanisms. -
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. -
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 Gyrase/Topoisomerase Inhibitor
Levofloxacin mesylate is a potent DNA gyrase and topoisomerase IV inhibitor. As an orally active antibiotic, it exhibits significant antibacterial activity against both Gram-positive and Gram-negative bacteria. This compound is applicable in various research contexts, including studies on chronic periodontitis, airway inflammation, and BK viremia. Additionally, levofloxacin mesylate demonstrates anti-orthopoxvirus properties, making it valuable for investigations into viral infections. -
Topoisomerase Inhibitor
OSUAB-0284 is a potent bacterial topoisomerase inhibitor, exhibiting significant anti-staphylococcal activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA). By targeting and inhibiting bacterial topoisomerase, OSUAB-0284 effectively disrupts bacterial DNA replication and transcription processes. This compound is valuable for researching infections linked to drug-resistant bacteria, providing insights into potential therapeutic strategies against MRSA and other related pathogens. -
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. -
Endogenous Ceramide
Ceramides Mixture consists of endogenous ceramides, including hydroxy and non-hydroxy fatty acid-containing variants. It plays a crucial role in maintaining the permeability barrier of the epidermis. This mixture is involved in key biological activities such as growth inhibition, cell cycle arrest, and modulation of telomerase activity, making it valuable for research applications focused on skin physiology, aging, and cellular signaling pathways. -
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. -
Telomerase Inhibitor
Telomerase-IN-2 is a telomerase inhibitor that functions by reducing the expression of dyskerin, effectively decreasing telomerase activity with an IC50 of 0.89 µM. This compound has demonstrated promising anti-cancer activity, making it a valuable tool for research into telomerase-related cancer therapeutics and cellular aging studies. Its ability to target telomerase presents potential applications in cancer biology and therapies aimed at inhibiting tumor proliferation. -
Prokaryotic Telomerase
TelN Protelomerase is a prokaryotic telomerase derived from bacteriophage N15 that exhibits cleaving-joining activity essential for the synthesis of linear prophage DNA with terminally closed ends in lysogenic bacteria. This enzyme functions by cleaving both strands of DNA and subsequently joining the ends to produce covalently closed hairpin structures. TelN Protelomerase is valuable for research applications involving bacteriophage biology, telomere dynamics, and the study of lysogenic conversion mechanisms. -
Telomerase Inhibitor
Telomerase-IN-8 is an orally active inhibitor of telomerase, exhibiting an IC50 of 0.98 μM. This compound demonstrates significant antiproliferative activity against various tumor cell lines, including PC3, Bcap-37, MGC-803, and HepG2. Additionally, Telomerase-IN-8 displays substantial antitumor efficacy in S180 sarcoma and HepG2 hepatoma xenograft models. It serves as a valuable tool for investigating telomerase-targeted approaches in cancer research. -
Telomerase Inhibitor
Telomerase-IN-7 is a potent telomerase inhibitor with an IC50 of 0.03 μM. By selectively targeting the telomerase enzyme, it effectively impedes cellular proliferation associated with various cancers. This compound is applicable in cancer research, particularly in studies focusing on telomere biology and cellular aging mechanisms. -
Telomerase Inhibitor
7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP) is a nucleotide analogue that serves as an effective telomerase inhibitor, with an IC50 of 11 μM. This compound is utilized in various research applications to study telomere biology and elucidate the mechanisms of telomerase activity. Its unique structure allows for the exploration of telomerase's role in cellular aging and cancer development. -
Telomerase Inhibitor
FJ-5002 is a potent telomerase inhibitor with an IC50 of 2 μM. It effectively induces telomere shortening and leads to increased chromosomal abnormalities, as well as senescence-like features in the human leukemia cell line U937. This compound exhibits significant antitumor activity, making it an important tool in cancer research and the study of telomerase-related mechanisms in tumorigenesis. -
PROTAC Target Protein Ligand
TERT ligand-1 is a PROTAC target protein ligand that facilitates the synthesis of the PROTAC NU-PRO-1. This compound has shown efficacy in inducing degradation of telomerase reverse transcriptase (TERT) in cancer cells. TERT ligand-1 is instrumental in research applications focused on targeted protein degradation and cancer therapeutics development. -
Telomerase Inhibitor
3′-Azido-2′,3′-dideoxy-GTP (AZddGTP) is a selective inhibitor of telomerase, exhibiting a Ki value of 1.5 μM. This compound can be incorporated into the 3′-terminus of DNA by telomerase, leading to the inhibition of telomerase activity. Research applications include studying telomerase function and its role in cellular aging and cancer biology, particularly in HeLa cells in vitro. -
TERT Activator
TERT Activator-2 is a selective activator of telomerase reverse transcriptase (TERT), known to enhance the expression of TERT in cellular models. This compound is instrumental in studies focused on telomere maintenance and cellular lifespan, facilitating research into aging and age-related diseases. Its ability to modulate telomerase activity positions TERT Activator-2 as a valuable tool in the exploration of cellular senescence and regenerative medicine. -
Telomerase Inhibitor
Macrocalin B is a diterpenoid that acts as a potent telomerase inhibitor. This compound effectively inhibits the proliferation of various cancer cell lines, including K562, HL-60, A549, MKN, CA, and HCT, with IC50 values ranging from 2.81 to 171 μM. Notably, Macrocalin B demonstrates nanomolar level inhibition of telomerase in K562 cells. This makes it a valuable tool for research into cancer biology and potential therapeutic applications targeting telomerase activity. -
L2H2-6OTD Intermediate
L2H2-6OTD intermediate-2 is an intermediate in the synthesis of telomerase inhibitors, specifically designed for applications in antibody-drug conjugate (ADC) development. This compound plays a crucial role in enhancing the efficacy of targeted cancer therapies by inhibiting telomerase activity, thereby contributing to the selective cytotoxicity against tumor cells. Researchers can leverage this intermediate for further investigation into novel therapeutic strategies in cancer treatment. -
PBK Inhibitor
PBK-IN-9 is a potent inhibitor of PDZ binding kinase (PBK), a key regulator involved in various cellular processes. This compound demonstrates significant biological activity by inhibiting PBK's kinase activity, making it an essential tool for studying cellular signaling pathways and cancer biology. PBK-IN-9 is widely used in research applications focused on understanding the role of PBK in tumor progression and therapeutic resistance. -
TopI Inhibitor
(1R,9R)-Exatecan mesylate is a potent inhibitor of topoisomerase I, with an IC50 of 0.975 μg/mL in mice and 0.82 μg/mL in humans. This non-prodrug camptothecin derivative stabilizes the enzyme-DNA cleavable complex, effectively blocking topoisomerase I activity and inducing apoptosis. (1R,9R)-Exatecan mesylate demonstrates significant anti-proliferative effects on a variety of malignant tumor cells and addresses P-glycoprotein-mediated multidrug resistance. It is utilized in preclinical research across multiple cancer types, including pancreatic, lung, breast cancers, and leukemia. -
Top I Inhibitor
(1S,9R)-Exatecan mesylate is a potent topoisomerase I inhibitor that acts by stabilizing the enzyme-DNA cleavable complex, thereby blocking enzyme activity and inducing apoptosis. With an IC50 value of 0.975 μg/mL in mice and 0.82 μg/mL in humans, this non-prodrug camptothecin derivative effectively inhibits the proliferation of various malignant tumor cells and tumor growth while overcoming P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is utilized in preclinical studies on multiple cancers, including pancreatic, lung, breast cancers, and leukemia. -
Topoisomerase II Inhibitor
Merbarone is an orally active inhibitor of topoisomerase II, functioning primarily by obstructing the enzyme's capacity to mediate DNA cleavage without stabilizing the covalent complexes formed between topoisomerase II and DNA. As an anticancer agent, Merbarone demonstrates effective cytotoxicity in various cancer cell lines, making it a valuable tool for cancer research and therapeutic studies focused on topoisomerase-targeted therapies. -
TOP2A Transcriptional Inhibitor
PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). This compound effectively eliminates undifferentiated human pluripotent stem cells (hPSCs), making it a valuable tool for stem cell research and differentiation studies. Its ability to precisely target TOP2A provides researchers with a means to manipulate pluripotency and investigate cellular differentiation processes. -
Topoisomerase Inhibitor
Ellipticine hydrochloride is a potent topoisomerase II inhibitor, functioning as an effective antineoplastic agent. It disrupts DNA replication and transcription processes, leading to cytotoxic effects in rapidly dividing cells. This compound is utilized in cancer research to investigate mechanisms of tumorigenesis and therapeutic response. -
Anti-Cancer Agent
Coralyne chloride is a protoberberine alkaloid that functions as a potent anti-cancer agent by inhibiting topoisomerase I. It acts as a topoisomerase I poison, inducing DNA cleavage mediated by this enzyme. Coralyne chloride is also utilized in the preparation of coralyne derivatives, which serve as DNA-binding fluorescent probes, making it valuable for various research applications in cancer biology and molecular imaging. -
TOP2B Inhibitor
Topobexin is a selective inhibitor of Topoisomerase II beta (TOP2B), demonstrating an IC50 value of 0.19 μM for TOP2B and 4.8 μM for TOP2A in DNA decatenation assays. By binding to non-homologous residues within the obex pocket, Topobexin effectively targets the ATPase domain of TOP2B. This compound mitigates anthracycline-induced DNA double-strand breaks and associated apoptotic signaling without impairing the anticancer effects of anthracyclines in cancer cells. It serves as a valuable tool for research into anthracycline-induced cardiotoxicity, revealing insights into cellular stress responses and cardiac function.
