Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Purine Nucleoside Analog
3-O-(4-Methoxybenzyl)-4-C-hydroxymethyl-1,2-O-isopropylidine-alpha-D-ribofuranose is a purine nucleoside analog that exhibits significant anticancer activity. It primarily targets indolent lymphoid malignancies through mechanisms such as the inhibition of DNA synthesis and the induction of apoptosis. This compound is valuable for research focusing on cancer therapeutics and the underlying molecular pathways involved in tumor progression. -
Purine Nucleoside Analog
2′-Azido-5′-O-[bis(4-methoxyphenyl)phenylmethyl]-2′-deoxyuridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer effects are primarily due to the inhibition of DNA synthesis and the induction of apoptosis. Additionally, this compound serves as a versatile click chemistry reagent, incorporating an azide group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with alkyne-containing molecules, including those with DBCO or BCN moieties. -
Nucleoside Metabolite
(S)-5-Amino-3-oxohexanoic acid acts as a nucleoside metabolite with significant implications in biochemical research. This compound plays a role in metabolic pathways involving amino acid synthesis and nucleoside metabolism. It is utilized in studies of enzyme activity and may contribute to the understanding of metabolic disorders and nucleoside-related functions in cellular processes. -
Purine Nucleoside Analog
2’-O-Acetyl-5’-O-(p-toluoyl)-3’-deoxy-3’-fluoro-5-methyluridine is a purine nucleoside analog. This compound exhibits significant antitumor activity against indolent lymphoid malignancies by targeting DNA synthesis and inducing apoptotic pathways. Its unique mechanism of action makes it a valuable tool for cancer research and a promising candidate for therapeutic development. -
Purine Nucleoside Analog
Thymine 1-β-D-arabinofuranoside is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its mechanisms of action include the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable tool for cancer research. This compound is suitable for studies focused on the development and exploration of novel therapeutic strategies in oncology. -
Purine Nucleoside Analog
3’-O-MOE-5Me-C(Bz)-2’-phosphoramidite is a purine nucleoside analog that acts by targeting critical pathways involved in cancer biology. This compound exhibits broad antitumor activity, particularly against indolent lymphoid malignancies, by inhibiting DNA synthesis and inducing apoptosis in cancerous cells. It is a valuable reagent for researchers investigating therapeutic strategies in oncology and nucleic acid-based applications. -
Purine Nucleoside Analog
5-O-Benzoyl-1,2,3-tri-O-acetyl-4-C-methyl-D-ribofuranose is a purine nucleoside analog that demonstrates significant antitumor activity. This compound functions primarily by inhibiting DNA synthesis and inducing apoptosis, making it a valuable tool for research in cancer biology. It is particularly relevant for investigating treatments for indolent lymphoid malignancies and other related malignancies. -
Purine Nucleoside Analog
N1-(1,1,1-Trifluoroethyl)pseudouridine is a purine nucleoside analog that exerts its antitumor effects by inhibiting DNA synthesis and promoting apoptosis. This compound is primarily utilized in the research of indolent lymphoid malignancies, where it demonstrates significant potential for therapeutic applications. Its unique structure and biological activity make it a valuable tool for studying cancer cell proliferation and survival mechanisms. -
Nucleoside Metabolite
11,14,15-THETA (11,14,15-Trihydroxyeicosatrienoic acid) is a nucleoside metabolite known for its role in various biological processes. This compound exhibits significant bioactivity, influencing lipid signaling pathways and inflammatory responses. It is commonly utilized in research exploring metabolic pathways, inflammation, and cell signaling mechanisms. -
Adenosine Analog
8-Methylthio-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. It has demonstrated the potential to inhibit cancer progression, making it a valuable tool in cancer research and therapeutic investigations. This compound is relevant for studies exploring the biochemical pathways influenced by adenosine and its analogs. -
Guanosine Analog
1,2'-O-Dimethylguanosine is a guanosine analogue that primarily targets Toll-like receptor 7 (TLR7). It exhibits immunostimulatory activities and has been shown to induce type I interferons in certain animal models, leading to antiviral effects. This compound serves as a valuable tool in research focused on innate immunity and therapeutic applications in viral infections. -
Purine Nucleoside Analog
5’(R)-C-Methyl-3-deazauridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its primary mechanism involves the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable reagent for cancer research. This compound is suitable for studies focused on the mechanisms of action of nucleoside analogs and their therapeutic potential in oncology. -
Purine Nucleoside Analog
3’-Azido-3’-deoxy-5-iodouridine is a purine nucleoside analog that targets DNA synthesis pathways to exhibit antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer effects are primarily mediated through inhibition of DNA replication and the induction of apoptosis. Additionally, this compound serves as a versatile click chemistry reagent, featuring an azide group that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with alkyne, DBCO, or BCN-functionalized molecules. This makes it a valuable tool for bioconjugation applications in chemical biology research. -
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. -
HDAC Inhibitor
CM-444 is a potent inhibitor of histone deacetylases (HDACs) with an IC50 range of 6 nM to 0.6 μM, and demonstrates inhibition of DNA methyltransferases (DNMT) with IC50 values between 1.8 and 2.3 μM. This compound facilitates the differentiation of acute myeloid leukemia cells and exhibits significant anti-leukemic activity, enhancing survival rates in mouse models. CM-444 serves as a valuable tool for research into cancer epigenetics and the development of targeted therapies for leukemia. -
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. -
SIRT2 Inhibitor
RK-9123016 is a selective inhibitor of SIRT2, effectively inhibiting its enzymatic activity with an IC50 of 0.18 µM, while showing no significant effect on SIRT1 or SIRT3 at concentrations up to 100 µM. This compound enhances the acetylation of eukaryotic translation initiation factor 5A (eIF5A), a known substrate of SIRT2, and is shown to decrease cell viability in human breast cancer cells, correlating with reduced expression of c-Myc. RK-9123016 is valuable for research into cancer biology and the role of sirtuins in cellular processes. -
SIRT1 Activator
Altissimacoumarin F is a terpenylated coumarin that acts as an activator of SIRT1, a protein implicated in cellular stress response and longevity. This compound, isolated from the stem bark of Ailanthus altissima, enhances SIRT1 activity while simultaneously decreasing p53 transcriptional activity. Altissimacoumarin F is valuable for research into age-related disorders and related pathways, providing insights into potential therapeutic strategies. -
SIRT1 Inhibitor
SIRT1-IN-6 is a selective SIRT1 inhibitor with an IC50 value of 9.7 μM. This compound effectively increases p53 acetylation, which is significant in regulating cell cycle and apoptosis. SIRT1-IN-6 is ideal for research applications related to neurodegenerative diseases and cancer, offering insights into potential therapeutic strategies for these conditions. -
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. -
DNA Synthesis Inhibitor
Quinoprazine is a potent inhibitor of DNA synthesis, specifically targeting Vaccinia virus with an IC50 value of 10 μM. This compound demonstrates significant antimalarial activity against Plasmodium berghei and exhibits antiprion efficacy, effectively reducing levels of the pathogenic protein PrPSc. Quinoprazine's diverse biological activities make it a valuable tool for research in virology, parasitology, and prion disease studies. -
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. -
RSV Polymerase inhibitor
RSV L-protein-IN-3 is an inhibitor of respiratory syncytial virus (RSV) polymerase, displaying an IC50 value of 10.4 μM and an EC50 value of 2.1 μM against RSV. It demonstrates reduced cytotoxicity compared to the clinical agent Ribavirin, making it a suitable candidate for further research into treating RSV infections. This compound is valuable for studies focusing on antiviral mechanisms and drug development targeting RSV. -
RSV Polymerase Inhibitor
RSV L-protein-IN-4 is a noncompetitive inhibitor of the respiratory syncytial virus (RSV) polymerase, exhibiting an IC50 value of 0.88 μM. This compound demonstrates significant antiviral activity against various RSV strains, with an EC50 of 0.25 μM. RSV L-protein-IN-4 is essential for research into antiviral therapies targeting RSV infections. -
RSV Polymerase Inhibitor
RSV L-protein-IN-2 is a noncompetitive inhibitor of the Respiratory Syncytial Virus (RSV) polymerase, exhibiting an IC50 value of 4.5 μM. This compound demonstrates significant antiviral activity against long strains of RSV, with an EC50 of 1.3 μM. It is applicable in research focused on developing therapeutic strategies against RSV infections and understanding viral replication mechanisms. -
RNA-dependent RNA Polymerase Inhibitor
BPR3P0128 is a non-nucleoside inhibitor of RNA-dependent RNA polymerase (RdRp), demonstrating potent antiviral activity against various SARS-CoV-2 variants. It exhibits EC50 values of 0.62 μM for SARS-CoV-2 and 0.14 μM for HCoV-229E, effectively inhibiting virus replication within the submicromolar range. Additionally, BPR3P0128 shows synergistic effects when used in combination with Remdesivir, making it a promising candidate for further antiviral research against coronaviruses. -
Anti-HIV-1 Nucleoside Analog
QYL-685 is an anti-HIV-1 nucleoside analog featuring a Z-methenylcyclopropane structure with 2,6-diaminopurine, demonstrating significant antiviral activity against HIV-1. This compound is effective against HIV-1 strains resistant to Zidovudine and Didanosine in vitro. QYL-685 serves as a valuable tool for researching HIV-1 infection and evaluating antiviral mechanisms. -
Oxathiolane Nucleoside Analog
rel-Emtricitabine is an oxathiolane nucleoside analog primarily targeting reverse transcriptase in HIV. It exhibits potent antiviral activity against HIV, making it an essential component of combination therapy for effectively managing HIV infections. This compound is valuable for research applications focused on HIV replication and therapeutic strategies. -
Nucleoside Analog
N6-Benzoyl-2'-deoxyadenosine monohydrate is a nucleoside analog that interacts with DNA duplexes, resulting in structural alterations. This modification can be utilized in the diagnosis of bacterial infections, with detection methods often employing electrophoresis. Its ability to bind to and perturb DNA structures makes it valuable for research in molecular biology and nucleic acid studies.
