Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Topoisomerase II Inhibitor
Bimolane, a potent inhibitor of human topoisomerase II, serves as an important tool in cancer research and therapy. This compound exhibits anti-neoplastic properties and has been investigated for its potential applications in psoriasis research. Additionally, Bimolane has demonstrated leukemogenic activity and the ability to induce various chromosomal aberrations in human lymphocytes, making it valuable for studies on genomic instability. -
TOP3B Inhibitor
TOP3B-IN-1 is a selective inhibitor of Topoisomerase IIIβ (TOP3B), disrupting the formation of TOP3B cleavage complexes (TOP3Bccs) with DNA and RNA. This compound destabilizes existing TOP3Bccs, making it valuable for investigating the role of TOP3B in cellular processes. TOP3B-IN-1 serves as a useful control in the development of new TOP3B-targeting inhibitors, allowing for enhanced understanding of this enzyme’s function in biological systems. -
Topoisomerase Inhibitor
Topoisomerase II inhibitor 1 is a selective inhibitor targeting topoisomerase IIα, a critical enzyme involved in DNA replication and cell division. This compound demonstrates potent biological activity in disrupting DNA topology, leading to the prevention of DNA strand separation. It is utilized in research applications focused on cancer biology and the development of anti-cancer therapeutics, particularly in studies examining DNA repair mechanisms and cellular proliferation. -
Anti-leukemia Compound
Moflomycin is a potent anti-leukemia compound that exhibits strong antiproliferative effects, particularly against the HL60 leukemic cell line, with an IC50 of 2.9 nM. Its mechanism involves enhancing topoisomerase II-induced DNA breaks and stimulating free radical production. Moflomycin presents valuable opportunities for research applications in leukemia treatment and drug development. -
Topoisomerase I Inhibitor
10-Nitrocamptothecin is a potent inhibitor of topoisomerase I, exhibiting an IC50 value of 0.64 μM. This compound disrupts the formation of cleavable complexes, thereby effectively inhibiting topoisomerase I activity. It is widely utilized in cancer research to explore therapeutic strategies targeting DNA replication and repair mechanisms. -
topoisomerase I/II Inhibitor
XR11576 is an orally active inhibitor of topoisomerase I and II, demonstrating significant cytotoxicity against both human and murine tumor cell lines, with IC50 values ranging from 6 to 47 nM. This compound is primarily utilized in cancer research to explore the mechanisms of DNA replication and repair, making it a valuable tool for investigations into anticancer therapies and the underlying biology of tumor cells. -
DNA Topoisomerase Inhibitor
BE-10988 is a potent DNA topoisomerase inhibitor that disrupts the normal function of this enzyme, leading to the formation of stabilized enzyme-DNA complexes. This compound effectively inhibits the growth of Doxorubicin- and vincristine-resistant P388 mouse leukemia cell lines, indicating its potential utility in overcoming drug resistance in cancer treatment. BE-10988 offers valuable insights for research in cancer biology and therapeutic development. -
TopoI Inhibitor
GI-149893 is a selective topoisomerase I (TopoI) inhibitor that disrupts the religation of DNA, leading to irreversible DNA damage in tumor cells. This compound demonstrates significant cytotoxic effects against various cancer cell lines, including colon carcinoma (HT-29/SW-48), breast cancer (MX-1), and prostate cancer xenografts (PC-3). GI-149893 serves as a valuable tool for cancer research, particularly in the exploration of therapeutic strategies targeting TopoI. -
Anticancer Agent
Tenifatecan is an injectable emulsion designed primarily as an anticancer agent. It consists of vitamin E and a succinate derivative, along with 7-ethyl-10-hydroxycamptothecin (SN-38), which is the active metabolite of irinotecan. Tenifatecan exhibits potent anticancer activity, making it a valuable compound for research applications in cancer therapy and drug development. -
Doxorubicin Analog
Camsirubicin is a non-cardiotoxic analog of Doxorubicin that selectively targets topoisomerase IIβ. This compound demonstrates significant anti-proliferative effects, reducing cell viability and clone formation in MDA-MB-468 breast cancer cells. Furthermore, Camsirubicin enhances the surface exposure of calreticulin (CALR) and heat shock protein 90 (HSP90). It is an effective reagent for studies focused on breast cancer biology and therapeutic strategies. -
Topoisomerase Inhibitor
S 39625 is a camptothecin ketone analogue that functions as a selective inhibitor of topoisomerase I. This compound exhibits potent activity against purified topoisomerase I and demonstrates cytotoxic effects in cancer cells. It is a valuable reagent for research applications involving cancer biology and the study of topoisomerase inhibition mechanisms. -
Topoisomerase
Ro 47-3359 is a pyrimido[1,6-a]benzimidazole compound that specifically enhances the activity of eukaryotic topoisomerase II, promoting DNA cleavage. This compound has demonstrated cytotoxic effects in Kc cells, making it a valuable tool for studying topoisomerase function and the mechanisms underlying cellular response to DNA damage. Ro 47-3359 is relevant for research applications in cancer biology and DNA repair pathways. -
DNA topoisomerase I Inhibitor
9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a potent inhibitor of DNA topoisomerase I, a key enzyme involved in DNA replication and transcription. This compound exhibits significant anticancer activity by inducing DNA damage through the stabilization of the enzyme-DNA cleavable complex. It is particularly useful in cancer research for studying the mechanisms of tumor progression and therapy resistance, as well as evaluating potential chemotherapeutic strategies. -
DNA Topoisomerases I/II Inhibitor
Nectandrin B is an inhibitor of DNA topoisomerases I and II, derived from Saururus chinensis. It exhibits significant potential in cancer research by disrupting the topoisomerase activity essential for DNA replication and repair. This compound serves as a valuable tool for investigating the therapeutic mechanisms and efficacy of topoisomerase-targeted treatments in oncology. -
Topoisomerase II-Targeted Agent
CP-67804 is a quinolone derivative that targets topoisomerase II. This compound effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II, showcasing its potential as an antineoplastic agent. CP-67804 is suitable for research applications focused on cancer biology and DNA topology. -
Topoisomerase II Inhibitor
Pixantrone hydrochloride is a topoisomerase II inhibitor that functions through DNA intercalation, exhibiting significant anti-tumor activity. It is a structural analog of mitoxantrone and has shown promise in preclinical and clinical studies for treating various malignancies. This compound is valuable for research applications in cancer biology, particularly in studies focused on the mechanisms of DNA damage and repair, as well as the assessment of therapeutic efficacy in oncology. -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 4 (compound E17) targets the topoisomerase II enzyme, disrupting DNA replication and repair processes. It is characterized by its ability to induce G2/M cell cycle arrest, demonstrating significant anti-tumor activity through potent cytotoxic and anti-proliferative effects. This compound is suitable for research applications focused on cancer biology and therapeutic development. -
Topoisomerase Inhibitor
Topotecan acetate is a topoisomerase inhibitor that functions by stabilizing the topoisomerase-DNA complex during DNA replication, ultimately leading to DNA damage and cell death. This compound demonstrates potent antitumor activity, particularly in the treatment of ovarian and small cell lung cancers. Topotecan acetate is utilized in various research applications to study cellular responses to DNA damage and to evaluate potential therapeutic strategies in oncology. -
Topo IIα Inhibitor
Topoisomerase IIα-IN-2 is a potent inhibitor of topoisomerase IIα, targeting the enzyme's DNA-binding activity. It demonstrates significant antiproliferative effects against various human cancer cell lines and induces substantial DNA damage. Additionally, Topoisomerase IIα-IN-2 effectively halts cancer cell progression at the G2/M phase, making it a valuable reagent for cancer research and therapeutic investigations. -
Topo I inhibitor
Fagopyrine is a potent inhibitor of DNA topoisomerase I (Topo I), an enzyme critical for DNA relaxation and transcription processes. Its ability to intercalate into DNA makes Fagopyrine a valuable tool in cancer research, particularly in studies involving tumor dynamics and photosensitization therapies. This compound can be instrumental in understanding the role of Topo I in tumor cell proliferation and response to treatment. -
Topoisomerase Inhibitor
A 9387 is a topoisomerase inhibitor that specifically targets Tn3 Resolvase, interrupting its role in site-specific recombination between directly repeated sequences. This compound effectively inhibits the binding of resolvase to the resolution site, thereby preventing the recombination process. A 9387 is valuable for research applications in genetic recombination and molecular biology studies focused on DNA manipulation and topological changes. -
Topoisomerase I Inhibitor
β-Glu-PAB(CH2NH2)-Exatecan is a selective inhibitor of topoisomerase I. It disrupts the topoisomerase I-DNA complex, preventing DNA strand rejoining, which leads to DNA breakage and subsequent apoptosis in cancer cells. This compound is specifically designed to be activated by β-glucuronidase, which is highly expressed in the tumor microenvironment, thereby activating Exatecan and enhancing its cytotoxicity. β-Glu-PAB(CH2NH2)-Exatecan serves as a valuable tool for cancer research, particularly in exploring targeted therapies. -
Topoisomerase I Inhibitor
Topoisomerase I-IN-19 is a potent inhibitor of Topoisomerase I, a critical enzyme involved in DNA replication and transcription. This compound facilitates the study of Topoisomerase I-mediated diseases, particularly in cancer research, by allowing for the evaluation of cell growth, apoptosis, and the therapeutic potential of Topoisomerase I inhibition. Its efficacy in modulating Topoisomerase I activity makes it a valuable tool for mechanistic studies and drug development in oncology. -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 18 is a quinoxaline derivative that selectively inhibits topoisomerase II with an IC50 of 7.5 μM. This compound effectively suppresses cell proliferation and induces G1/S phase cell cycle arrest, leading to apoptosis in PC-3 cancer cells. It demonstrates significant antitumor activity, making it a valuable tool for cancer research applications focused on topoisomerase II modulation. -
DNA Topoisomerase Inhibitor
PNU-142586 sodium is a potent inhibitor of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). This compound effectively disrupts DNA replication and transcription by preventing the binding of DNA to TOP2 and inhibiting ATP hydrolysis, resulting in antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 sodium is primarily utilized in research investigating Linezolid-induced hematotoxicity and its underlying molecular mechanisms. -
Antitumor Agent
Piroxantrone is a potent anthrapyrazole antitumor agent that primarily targets DNA topoisomerase II. It exhibits significant cytotoxic effects on cancer cells, making it a valuable compound for research in oncological studies. However, it is important to note that Piroxantrone also displays cardiotoxicity, highlighting the need for careful evaluation in therapeutic applications. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 6 is a potent and selective inhibitor of topoisomerase II, derived from tryptanthrin. This compound demonstrates significant antiproliferative activity across various tumor cell lines and effectively halts the cell cycle of CCRF-CEM cells at the G2 phase, while inducing DNA double-strand breaks (DSBs). Its robust mechanism of action makes Topoisomerase II inhibitor 6 a valuable reagent for cancer research and therapeutic investigations. -
Topoisomerase Inhibitor
Amonafide dihydrochloride is a potent inhibitor of topoisomerase II, functioning by disrupting the enzyme's binding to DNA and subsequently halting DNA and RNA synthesis. This compound exhibits significant cytotoxicity and is capable of inducing apoptotic signaling pathways. Notably, Amonafide dihydrochloride retains its efficacy in the context of P-glycoprotein-mediated multidrug resistance, making it a valuable tool for cancer research and development of therapies targeting resistant tumors. -
Resolvase Inhibitor
A1062 is a potent inhibitor of Tn3-encoded resolvase, exhibiting an IC50 in the micromolar range. This compound effectively suppresses the binding of resolvase proteins to their respective sites, thereby blocking resolvase-induced site-specific recombination. A1062 can be utilized in research applications focused on understanding site-specific recombination mechanisms and exploring genetic engineering strategies. -
DNA Topoisomerase Inhibitor
Pazelliptine is a potent DNA topoisomerase inhibitor that exhibits significant antitumor activity. By interfering with the enzyme's action, Pazelliptine can induce DNA damage and inhibit cellular proliferation, making it a valuable tool in cancer research. Its ability to disrupt critical cellular processes positions it as an important reagent for studying mechanisms of tumorigenesis and developing therapeutic strategies. -
Topoisomerase II Inhibitor
ARN24139 is a potent inhibitor of topoisomerase II, exhibiting an IC50 value of 7.3 μM. This compound demonstrates significant anti-proliferative effects on cancer cells and has shown an acceptable safety profile in vivo. ARN24139 is suitable for use in studies focused on cancer biology and therapeutic development targeting topoisomerase II-mediated pathways. -
Anticancer agent
Anticancer agent 216 (34A) is a Camptothecin derivative that selectively inhibits topoisomerase I, disrupting DNA replication and transcription. It demonstrates potent cytotoxicity with IC50 values of 9.6 nM in MCF-7 breast cancer cells and 11.6 nM in MDA-MB-231 cells. This compound is valuable for research applications focused on developing targeted therapies for breast cancer and understanding the mechanisms of tumor cell resistance. -
Topoisomerases I/II Inhibitor
Elomotecan is a potent inhibitor of topoisomerases I and II, classified as a camptothecin analog within the homocamptothecin family. This compound exhibits significant cytotoxic activity against various tumor cell lines, demonstrating enhanced efficacy compared to standard anticancer agents targeting the same mechanisms. Elomotecan's ability to interfere with DNA replication and repair makes it a valuable tool in cancer research and drug development. -
Antitumor Drug
Atiratecan is a proagent of the camptothecin analog CH0793076, primarily targeting tumor cells. It demonstrates significant antitumor activity in both breast cancer resistance protein (BCRP)-positive and -negative xenograft models in mice. Atiratecan is a valuable compound for research applications in cancer biology, particularly in exploring drug resistance mechanisms and developing new therapeutic strategies. -
DNA topoisomerase II Inhibitor
cis-THSG is a selective inhibitor of DNA topoisomerase II, demonstrating no activity against DNA topoisomerase I. This compound effectively suppresses the transcription of phosphoenolpyruvate carboxykinase (PEPCK), leading to reductions in blood glucose levels, improvement of glucose intolerance, and alleviation of insulin resistance in high-fat diet-induced diabetic male CF-1 mice. cis-THSG serves as a valuable tool for research into type 2 diabetes mellitus and the mechanisms of glucose metabolism. -
DNA Topoisomerase Inhibitor
Melicopidine is a DNA topoisomerase inhibitor derived from the acridone alkaloid family, sourced from the bark of Medicosma subsessilis. This compound demonstrates potential antitumor activity by binding to DNA and inhibiting the enzymatic activity of topoisomerases. It is applicable in various cancer research studies focusing on mechanisms of action related to DNA manipulation and repair processes. -
Topoisomerase-Ι Inhibitor
Camptothecin-20(S)-O-propionate hydrate is a potent topoisomerase I inhibitor. This compound is recognized for its significant anticancer properties, engaging in the modulation of DNA topology and inducing apoptosis in cancer cells. It is widely used in cancer research to explore mechanisms of chemotherapeutic action and to develop novel therapeutic strategies targeting topoisomerase I. -
Top I Inhibitor
BMS-250749 is a potent inhibitor of topoisomerase I (Top I) derived from the fluoroglycosyl-3,9-difluoroindolecarbazole class. It demonstrates significant cytotoxic effects and selectivity, exhibiting notable antitumor activity in Lewis lung cancer models. Additionally, BMS-250749 has shown broad-spectrum antitumor efficacy, outperforming CPT-11 in select preclinical xenograft studies. -
Topo II Inhibitor
Salvicine is a potent inhibitor of DNA topoisomerase II, exhibiting an IC50 of 3 μM. By targeting the ATPase domain of Topo II, Salvicine enhances its interaction with DNA, thereby inhibiting DNA degradation and ATP hydrolysis. This compound demonstrates significant anticancer properties, including the induction of DNA damage, the potential to overcome multidrug resistance, and the inhibition of tumor cell adhesion, making it a valuable tool for cancer research applications. -
Topoisomerase
(-)-Eleutherin is a pyranonaphthoquinone derivative that primarily targets DNA topoisomerase II, exhibiting potent cytotoxic activity. This compound induces significant DNA fragmentation, highlighting its efficacy in disrupting cellular integrity. Furthermore, (-)-Eleutherin demonstrates enhanced antioxidant properties, which may contribute to its therapeutic potential in various medicinal applications, making it a valuable candidate for cancer research and treatment strategies. -
Top II Inhibitor
A-74932 hydrochloride is a potent inhibitor of DNA topoisomerase II, a critical enzyme involved in DNA replication and transcription. By inhibiting the catalytic activity of mammalian topoisomerase II, A-74932 hydrochloride demonstrates significant antitumor activity. This compound is valuable for cancer research, particularly in studies focused on the modulation of topoisomerase function and the development of novel therapeutic strategies. -
Topoisomerase I Inhibitor
(±)-E-Homocamptothecin is a potent inhibitor of topoisomerase I, an enzyme critically involved in DNA replication and transcription. This compound is primarily utilized in cancer research, demonstrating significant potential in the study of tumor cell proliferation and resistance mechanisms. Its ability to interfere with DNA topology makes it a valuable tool in the exploration of therapeutic strategies targeting malignant cells. -
Anticancer agent
Anticancer agent 217 is a Camptothecin derivative targeting topoisomerase I, a crucial enzyme involved in DNA replication and repair. It demonstrates potent antitumor activity, with IC50 values of 6.2 nM in MCF-7 cells and 7.1 nM in MDA-MB-231 cells. This compound is suitable for research applications in cancer biology, particularly for studying the mechanisms of tumor cell proliferation and apoptosis.
