Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Camptothecin Derivative
7-Ethylcamptothecin is a derivative of Camptothecin and functions primarily as a DNA topoisomerase I inhibitor. This compound demonstrates considerable antitumor activity against various tumor cell lines, making it an important tool in cancer research. Additionally, 7-Ethylcamptothecin serves as a crucial precursor for the synthesis of 20 (S)-O-substituted benzoyl-7-ethylcamptothecin compounds, facilitating further exploration of potential therapeutic agents in oncology. -
Topoisomerase I/II Inhibitor
DACA is a potent inhibitor of topoisomerase I and II, capable of penetrating the blood-brain barrier. It demonstrates significant activity against various cancer types, including colorectal cancer, leukemia, and lung cancer. This compound serves as a valuable tool for investigating the mechanisms of these diseases and developing targeted therapies. -
Topoisomerase Inhibitor
LMP744 is a potent Topoisomerase I (Top1) inhibitor that functions as a DNA intercalator, disrupting the DNA replication process. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research. LMP744 can be utilized to study the mechanisms of Top1 inhibition and its effects on cell proliferation and apoptosis in various cancer models. -
TOP2 Inhibitor
T638 is a potent inhibitor of topoisomerase II (TOP2), demonstrating an IC50 of 0.7 µM against TOP2A activity. This compound exhibits significant anti-proliferative effects on cancer cells, making it a valuable tool for cancer research. Its ability to selectively disrupt topoisomerase activity positions T638 as an important reagent for investigating mechanisms of tumor growth and exploring potential therapeutic strategies. -
Topoisomerase IIα Inhibitor
ARN-21934 is a selective inhibitor of human topoisomerase IIα, effectively crossing the blood-brain barrier. It demonstrates potent inhibition of DNA relaxation, with an IC50 value of 2 μM, significantly outperforming Etoposide (IC50 = 120 μM). Due to its favorable in vivo pharmacokinetic properties, ARN-21934 is a promising candidate for further anticancer research and therapeutic development. -
Topoisomerase I Inhibitor
LMP744 hydrochloride is a potent Topoisomerase I inhibitor that functions as a DNA intercalator, disrupting the normal processes of DNA replication and transcription. This compound exhibits significant antitumor activity, making it a valuable tool in cancer research. Its ability to inhibit Topoisomerase I highlights its potential applications in studies targeting DNA damage response and therapeutic resistance in various malignancies. -
Antidiabetic/Antioxidant/Anitcancer Agent
Quercetin-3'-O-glucoside is a flavonoid glycoside that exhibits antidiabetic, antioxidant, and anticancer activities. It reduces liver glucose-6-phosphatase activity, modulates insulin and glucose levels, and enhances antioxidant enzyme functions in liver and kidney tissues. In cancer research, Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest, and promotes caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Additionally, it selectively disrupts EGFR-mediated signaling pathways and inhibits the migration and invasion of pancreatic cancer cells. This compound is valuable for studies focused on pancreatic cancer, diabetes, hepatocellular carcinoma, and other malignancies. -
Antitumor Agent
Bisantrene dihydrochloride is an effective antitumor agent that acts primarily through DNA intercalation. It specifically targets eukaryotic type II topoisomerases, disrupting DNA replication and transcription. Furthermore, Bisantrene dihydrochloride is a substrate of the multidrug resistance protein, MDR1, making it a relevant compound for studies on drug resistance mechanisms in cancer research. -
Top1 Inhibitor
Indimitecan is a topoisomerase I (Top1) inhibitor that exhibits potent anticancer activity. By disrupting DNA replication and transcription processes, it effectively impedes the proliferation of cancer cells. This compound is primarily utilized in cancer research, particularly for studies focused on therapeutic strategies targeting Top1. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
Camptothecin Derivative
12-Ethyl-9-hydroxycamptothecin is a derivative of camptothecin that functions primarily as a DNA topoisomerase I inhibitor. With an IC50 value of 679 nM, it displays significant biological activity in impairing DNA replication and transcription. This reagent is utilized in research applications focused on cancer therapeutics and the study of cell cycle regulation. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 13 acts as a selective inhibitor of topoisomerase II, a crucial enzyme involved in DNA replication and repair. This compound demonstrates potent antiproliferative activity against various cancer cell lines, effectively inducing apoptosis in cancer cells. It is valuable for research in cancer biology and therapeutic development targeting topoisomerase II-mediated pathways. -
Topoisomerase I Inhibitor
Lurtotecan is a semisynthetic analog of Camptothecin that functions as a topoisomerase I inhibitor. This compound exhibits significant anticancer properties, making it valuable for research in cancer therapy. Its ability to interfere with DNA replication and transcription positions it as a critical tool in the study of cancer cell mechanisms and drug resistance. -
Topoisomerase I Inhbitor
Topoisomerase I inhibitor 8 targets topoisomerase I, functioning as a potent inhibitor of this enzyme. This compound is a hexacyclic analogue of camptothecin and demonstrates significant cytotoxicity against tumor cells. It is suitable for research applications involving cancer biology and drug development, particularly in studies focused on DNA damage and repair mechanisms. -
Topoisomerases I and II Inhibitor
Elomotecan hydrochloride is a potent inhibitor of topoisomerases I and II, classified as a camptothecin analog from the homocamptothecin family. This compound demonstrates significant anti-proliferative activity in various tumor cell lines, surpassing the effectiveness of other known anticancer agents targeting these topoisomerases. Its mechanism of action makes Elomotecan hydrochloride a valuable tool in cancer research, particularly in studies focusing on DNA damage response and cell cycle regulation. -
Topoisomerase Inhibitor
Camptothecin-20(S)-O-propionate is a potent topoisomerase I inhibitor known for its significant anticancer properties. It impedes DNA replication and transcription by stabilizing the topoisomerase I-DNA complex, leading to cell cycle arrest and apoptosis in cancer cells. This compound is primarily utilized in cancer research to explore therapeutic strategies and efficacy in various malignancies. -
Topo II Inhibitor
9-Hydroxyellipticine hydrochloride is a potent inhibitor of topoisomerase II, targeting this essential enzyme involved in DNA replication and repair. This compound demonstrates significant antitumor activity, alongside antioxidant properties and catecholamine-releasing effects. In vitro studies reveal IC50 values of 1.6 μM and 1.2 μM in HeLa S-3 and 293T cell lines, respectively, highlighting its potential for cancer research applications. -
Topoisomerase II Inhibitor
Sobuzoxane is a potent topoisomerase II inhibitor that exerts its effects through the irreversible inhibition of cell division. This compound has demonstrated significant activity against non-Hodgkin's lymphoma, particularly in cases resistant to standard chemotherapy or in relapsed scenarios. It serves as an important tool for researchers exploring new treatment strategies for challenging hematological malignancies. -
Topoisomerase II Inhibitor
Razoxane is a topoisomerase II inhibitor known for its antiangiogenic properties. It exhibits significant antineoplastic and antimetastatic activities, making it a valuable tool in cancer research. Razoxane is particularly relevant for studies focusing on renal cell carcinoma (RCC), lung cancer, and melanoma, offering insights into tumor growth and metastasis mechanisms. -
TopI Inhibitor
20-O-Acetylcamptothecin is a potent inhibitor of Topoisomerase I, derived from the natural alkaloid Camptothecin. This compound exhibits significant antitumor activity by stabilizing the DNA-topoisomerase complex, leading to DNA strand breaks and subsequent cell death. It is widely utilized in cancer research to elucidate mechanisms of action and to explore therapeutic strategies targeting Topoisomerase I in various malignancies. -
Bioactive Component
1,4-Di-tert-butylbenzene is a bioactive compound known for its inhibitory effects on bacterial type II topoisomerases, specifically 4PLB and LpxC, as demonstrated in docking studies. This compound has potential applications in antibacterial research, providing a valuable tool for investigating mechanisms of resistance and developing new therapeutic strategies. Its presence in natural sources such as corn cob and green millet underscores its relevance in phytochemical studies. -
Top1 Inhibitor
meso-Tetra(4-pyridyl)porphine is a porphyrin derivative that acts as a weak inhibitor of human topoisomerase I (Top1), with an EC50 value exceeding 50 µM. This compound is of interest in tumor research, enabling investigations into the role of Top1 in cancer biology and potential therapeutic strategies. Its unique structural features make it a valuable tool for studying topoisomerase-related mechanisms in cellular processes. -
Anticancer Agent
Elinafide is an anticancer agent featuring a naphthalimide structure that targets DNA. It disrupts cellular metabolism by inserting a planar ring into the DNA double helix, leading to interactions with topoisomerase II enzymes. This mechanism results in significant cytotoxicity, with an IC50 value of 0.014 μM observed in HT-29 colorectal cancer cells. Elinafide is applicable for research on DNA-binding compounds and their therapeutic potential in oncology. -
TOP Inhibitor
PNU-142586 is an inhibitor of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B) that serves as a major metabolite of Linezolid. By obstructing the binding of DNA to topoisomerases and inhibiting ATP hydrolysis, PNU-142586 disrupts DNA replication and transcription, leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. This compound is valuable for investigating Linezolid-induced hematotoxicity and elucidating its underlying molecular mechanisms. -
Topoisomerase II Inhibitor
ARN21929 is an inhibitor of Topoisomerase II, exhibiting an IC50 value of 4.5 μM. This compound demonstrates favorable kinetic and thermodynamic solubility along with metabolic stability. Although ARN21929 shows limited antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cell lines, it remains a valuable tool for exploring mechanisms of cancer biology. -
Topoisomerase I Inhibitor
CH-0793076 is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 of 2.3 μM. This hexacyclic camptothecin analog serves as both an active drug and a significant metabolite of TP300. CH-0793076 demonstrates efficacy in cells that express the breast cancer resistance protein (BCRP), making it a valuable compound for investigating resistance mechanisms in oncology research. -
Topo II inhibitor
AQ4 is a topoisomerase II inhibitor and DNA intercalator that exhibits cytotoxic activity across various human tumor cell lines. This compound interferes with DNA replication and transcription, leading to cell cycle arrest and apoptosis. It is utilized in cancer research to study the mechanisms of DNA damage and the efficacy of potential therapeutic agents. -
Topoisomerase I Inhibitor
CH-0793076 TFA is a hexacyclic camptothecin analog that functions as a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 value of 2.3 μM. This compound demonstrates significant efficacy against tumor cells expressing the breast cancer resistance protein (BCRP). CH-0793076 TFA is primarily utilized in cancer research, particularly for studies focused on overcoming drug resistance in breast cancer and other malignancies where topoisomerase I plays a critical role. -
Topoisomerase I Inhibitor
Indotecan hydrochloride is a potent inhibitor of Topoisomerase I, demonstrating IC50 values of 300, 1200, and 560 nM in P388, HCT116, and MCF-7 cell lines, respectively. This indenoisoquinoline derivative functions by preventing the relaxation of supercoiled DNA, thus interfering with DNA replication and transcription processes. Indotecan hydrochloride has potential applications in cancer research and is also relevant in the study of visceral leishmaniasis. -
Topoisomerase Inhibitor
Silatecan is a topoisomerase I inhibitor that functions by interfering with DNA replication and transcription processes. As an analogue of Camptothecin, Silatecan exhibits enhanced stability and lipophilicity, making it a valuable agent for cancer research. Its notable antitumor properties and radiosensitizing effects contribute to its potential applications in oncology studies. -
DNA Topoisomerases I/II Inhibitor
Batracylin (NSC320846) is a potent inhibitor of DNA Topoisomerases I and II. It exhibits significant cytotoxic and antiproliferative effects, leading to the induction of DNA breaks in cellular systems. Batracylin is valuable for research applications focused on cancer biology, specifically in studies exploring the mechanisms of DNA damage and repair. -
Antitumor Agent
Sabarubicin is a doxorubicin disaccharide analogue that functions as an antitumor agent primarily through the inhibition of topoisomerase II. It demonstrates enhanced efficacy compared to doxorubicin, promoting DNA fragmentation at lower intracellular concentrations. This compound is valuable for researching mechanisms of cancer cell proliferation and apoptosis. -
Topoisomerase I Inhibitor
Diflomotecan is a potent inhibitor of topoisomerase I, exhibiting strong oral bioavailability. It demonstrates enhanced plasma stability and superior preclinical anti-tumor activity compared to established compounds. This makes Diflomotecan a valuable tool for cancer research and therapeutic development targeting topoisomerase I pathways. -
SN-38 Derivative
CL2-MMT-SN38 is a derivative of SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11). This compound exhibits potent anticancer activity by inducing DNA damage through the stabilization of the topoisomerase-DNA complex. Its unique structure makes it valuable for research applications focused on cancer therapeutics and the mechanistic understanding of topoisomerase inhibition. -
Antitumor Agent
Antitumor agent-63 is a 20 (S)-O-linked camptothecin (CPT) glycoconjugate predominantly targeting tumor cells while exhibiting minimal toxicity to normal cells. This compound demonstrates significant stability and presents very weak direct inhibition of topoisomerase I (Topo I). Its unique profile makes it a valuable candidate for research applications in cancer therapeutics and drug development. -
opoisomerase I Inhibitor T
Simmitecan hydrochloride is a potent inhibitor of topoisomerase I, derived from the 9-substituted lipophilic Camptothecin framework. This compound exhibits significant anticancer activity, making it a valuable reagent for cancer research. Simmitecan hydrochloride is utilized in studies focused on exploring mechanisms of tumor resistance and developing novel therapeutic strategies. -
Topoisomerase Inhibitor
CP-84364 is a potent topoisomerase I inhibitor that displays a dose-dependent inhibitory effect with an IC50 of 7.25 μg/mL. This compound shows significant antiproliferative and anticancer activities, making it valuable for cancer research and evaluating therapeutic strategies targeting topoisomerase I. Its ability to hinder cellular proliferation positions CP-84364 as a useful tool in the study of cancer biology and drug development. -
Doxorubicin Prodrug
SDOX is a doxorubicin prodrug designed to release the active compound doxorubicin in response to elevated levels of glutathione (GSH) found in tumor cells. This targeted mechanism minimizes adverse effects on healthy tissues while maintaining the therapeutic efficacy of doxorubicin. SDOX is suitable for research applications focused on cancer treatment and overcoming multidrug resistance. -
Anticancer Agent
Anticancer Agent 215 is a Camptothecin derivative that inhibits topoisomerase I activity. It demonstrates potent antiproliferative effects, with IC50 values of 5.2 nM in MCF-7 breast cancer cells and 8.2 nM in MDA-MB-231 cells. This compound is suited for cancer research applications, particularly in studies aimed at evaluating topoisomerase inhibition and exploring novel therapeutic strategies against breast cancer. -
Camptothecin Enantiomer
(R)-Camptothecin is the enantiomer of Camptothecin (CPT), specifically designed to lack inhibitory activity against DNA topoisomerase I (Top1). Due to its inability to hinder the DNA religation process, (R)-Camptothecin does not exhibit the cytotoxic properties characteristic of its active counterpart. This compound is primarily utilized in research applications focused on elucidating the mechanisms of action of camptothecin derivatives and understanding their pharmacological profiles.
