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Catalog No.
Product Name
Application
Product Information
Citations
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Topoisomerase Inhibitor
NBTIs-IN-6 is a potent bacterial topoisomerase inhibitor that exhibits significant antibacterial activity. Notably, it demonstrates an MIC90 of 2 μg/mL against fluoroquinolone-resistant Methicillin-resistant Staphylococcus aureus (MRSA). This compound is valuable for research applications aimed at understanding bacterial resistance mechanisms and developing new antimicrobial therapies. -
Topo II Inhibitor
Topoisomerase II inhibitor 12 is a selective inhibitor of topoisomerase II, functioning as a DNA non-intercalator. It exhibits significant antineoplastic activity, making it a valuable reagent in cancer research. This compound is suitable for studies focused on elucidating the mechanisms of action of topoisomerase II inhibitors and their therapeutic potential in oncology. -
DNA Topoisomerase I/II Inhibitor
Corydamine is a 3-arylisoquinoline alkaloid that serves as a potent inhibitor of DNA topoisomerase I and II. This compound exhibits significant anti-cancer activity and is utilized in research applications aimed at understanding the mechanisms of tumorigenesis and the development of targeted cancer therapies. Its ability to interfere with DNA manipulation makes it an important tool in the study of cellular processes and treatment modalities in oncology. -
Topoisomerase I Inhibitor
Topoisomerase I Inhibitor 4 is a selective inhibitor of topoisomerase I, effectively targeting the enzyme to disrupt DNA replication. It demonstrates significant anti-proliferative effects on various cancer cell lines, including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. This compound is valuable for cancer research, particularly in studying mechanisms of tumor growth inhibition. -
Topoisomerase II Inhibitor
Pericosine A is a potent inhibitor of topoisomerase II, derived from the Periconia byssoides strain. This compound exhibits significant antitumor activity, demonstrating efficacy in both in vitro and in vivo settings, making it a valuable tool in cancer research. Additionally, Pericosine A inhibits the epidermal growth factor receptor (EGFR) kinase, further expanding its potential applications in therapeutic research targeting malignancies. -
Topoisomerase-1 Inhibitor
TP3011 (CH0793011) is a potent topoisomerase I inhibitor, demonstrating equipotent activity comparable to SN38. It effectively inhibits the growth of various cancer cell lines, exhibiting IC50 values in the sub-nanomolar range in vitro. This compound is valuable for research applications focused on cancer therapy and the study of topoisomerase-targeted mechanisms. -
Topoisomerase Inhibitor
Topoisomerase Inhibitor 2 (18C) is a potent bacterial topoisomerase inhibitor, demonstrating broad-spectrum activity against multidrug-resistant Gram-negative bacteria. This reagent is valuable for research targeting bacterial DNA replication and repair pathways, making it relevant for studies focused on antibiotic resistance mechanisms and the development of novel antimicrobial agents. -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 8 is a potent inhibitor of topoisomerase II, demonstrating an IC50 of 0.52 μM. This compound exhibits significant anti-proliferative activity, effectively arresting the cell cycle at the G2/M phase. It is suitable for research applications involving cancer cell growth and the study of cell cycle regulation. -
Resolvase Inhibitor
A20832 is a selective inhibitor of resolvase, targeting its recombination and topoisomerase activities. This compound effectively disrupts the site-specific recombination mediated by the Tn3-encoded resolvase protein, specifically at the strand cleavage step, while leaving the synapsis process unaffected. A20832 serves as a valuable tool for researchers investigating the mechanisms of genetic recombination and the role of resolvase in various biological contexts. -
Topoisomerase II Inhibitor
Suptopin-2 is a potent inhibitor of topoisomerase II, a key enzyme involved in DNA replication and cell division. By inhibiting this target, Suptopin-2 disrupts cell cycle progression and destabilizes microtubules, leading to cell cycle arrest. This compound plays a crucial role in research focused on cancer biology and the mechanistic study of cellular processes involving nucleocytoplasmic transport, specifically through the regulation of cyclin B1. -
TopoII Inhibitor
Dichlorogelignate is a selective inhibitor of topoisomerase II (Topo II), demonstrating complete inhibition at a concentration of 50 μM. This compound is instrumental in studying the role of Topo II in DNA manipulation processes, making it valuable for cancer research and drug discovery applications targeting cellular proliferation and genomic stability. -
Topoisomerase I Inhibitor
Lurtotecan dihydrochloride is a semisynthetic analog of Camptothecin that acts as a topoisomerase I inhibitor. This compound exhibits significant anticancer activity, making it a valuable tool in cancer research. Its ability to interfere with DNA replication and transcription provides insights into tumor biology and therapeutic strategies. Researchers may utilize Lurtotecan dihydrochloride in studies of cancer cell survival, resistance mechanisms, and drug efficacy. -
Topoisomerase II Inhibitor
Bakuchicin, a topoisomerase II inhibitor derived from Psoralea corylifolia, demonstrates significant biological activity by inhibiting the enzyme's function. In cellular models infected with Simian virus 40 (SV40), Bakuchicin exhibits an IC50 value of 404 μM against topoisomerase II. This compound is primarily utilized in research focused on virology and anti-infection studies. -
Topoisomerase II Inhibitor
Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that serves as a moderate inhibitor of DNA topoisomerase II, with an IC50 value of 571 μM. This compound demonstrates notable cell growth inhibition, exhibiting IC50 values of 117 μM in K562 cells and 218 μM in CHO cells. Topoisomerase IIα-IN-9 is valuable for research applications focused on cancer biology and the mechanisms of drug resistance. -
topoisomerases I/II inhibitor
Becatecarin is an analog of rebeccamycin that primarily targets topoisomerases I and II. This compound exerts antitumor effects by intercalating into DNA, consequently inhibiting the catalytic activity of these enzymes. Due to its mechanism of action, Becatecarin is valuable in cancer research, particularly in studies exploring DNA damage and repair pathways. -
Topoisomerase II Inhibitor
8-Chloro-ATP tetrasodium is an analog of ATP that functions as an inhibitor of topoisomerase II (Topo II). It effectively inhibits DNA synthesis and promotes the formation of DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium also obstructs the ATP hydrolysis activity catalyzed by Topo II. This compound is valuable for research applications focused on cell division, DNA repair mechanisms, and topoisomerase function. -
Weak Inhibitor of Cell Proliferation
(S)-Gyramide A is a weak inhibitor of cell proliferation that targets DNA gyrase. Its primary biological activity involves interference with DNA supercoiling, which can disrupt bacterial cell division. Research applications of (S)-Gyramide A include studies on bacterial growth inhibition and the elucidation of the role of DNA gyrase in cell cycle regulation. This reagent is valuable for investigating potential antibacterial strategies and understanding the molecular mechanisms of cell proliferation. -
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. -
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. -
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. -
Chikungunya Virus Polymerase Inhibitor
GAP-1173149 is a selective inhibitor of the Chikungunya virus (CHIKV) polymerase, specifically targeting the nsP4 RNA-dependent RNA polymerase. This compound demonstrates potent antiviral activity by hindering viral RNA replication, making it a valuable tool for studying CHIKV biology and developing antiviral strategies. Its application is particularly relevant in research focused on emerging viral threats and potential therapeutic interventions for Chikungunya virus infections. -
SIRT1 Inhibitor
SIRT1-IN-1 is a selective inhibitor of SIRT1, exhibiting an IC50 of 0.205 μM. In addition to its primary target, it also inhibits SIRT2 with an IC50 of 11.5 μM. This indole compound demonstrates antiviral activity, particularly against cytomegalovirus (CMV), making it a valuable tool for research into SIRT1-related pathways and antiviral applications. -
Viral DNA Polymerases Inhibitor
Cidofovir diphosphate is a potent inhibitor of viral DNA polymerases, primarily targeting human cytomegalovirus (HCMV), herpes simplex virus type 1 (HSV-1), and herpes simplex virus type 2 (HSV-2). With Ki values of 6.6 μM, 0.86 μM, and 1.4 μM for these polymers, respectively, it demonstrates selective antiviral activity. This compound is instrumental in research focusing on antiviral drug development and elucidating the mechanisms underlying viral DNA replication. -
Polymerase Inhibitor
T-1105 is a novel broad-spectrum viral polymerase inhibitor that acts by being converted into a ribonucleoside triphosphate (RTP) metabolite. This compound demonstrates antiviral activity against multiple RNA viruses by inhibiting their polymerases. T-1105 is particularly significant in studies aimed at understanding viral replication and developing antiviral strategies. Its mechanism of action highlights its potential applications in viral pathogenesis research and therapeutic interventions. -
SIRT Inhibitor
Nicotinamide hydrochloride is an inhibitor of SIRT1 and SIRT2, targeting the sirtuin family of proteins critical for cellular regulation. This reagent has been shown to enhance cellular levels of NAD+ and ATP while increasing reactive oxygen species (ROS) levels. Research applications include investigation into tumor growth inhibition and potential improvements in survival, as well as exploring its anti-hepatitis B virus (HBV) activity. -
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 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. -
HCV NS5B Polymerase Inhibitor
MB-11362 is a potent, orally active inhibitor of the hepatitis C virus (HCV) NS5B polymerase, functioning as a 4′-azidouridine triphosphate prodrug. Upon oral administration, MB-11362 is converted to its active form, 4′-azidouridine triphosphate, which effectively disrupts viral RNA synthesis. This compound is valuable for research focusing on HCV infection and understanding the mechanisms of antiviral therapies targeting RNA polymerases. -
HCV RNA Polymerase Inhibitor
BILB 1941 is a potent nonnucleoside inhibitor targeting the hepatitis C virus (HCV) RNA polymerase. It demonstrates significant antiviral activity in vitro, making it a valuable tool for research applications related to HCV replication and drug development strategies against hepatitis C. -
NS5B Polymerase Inhibitor
ABT-072 potassium trihydrate is a potent non-nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase. It demonstrates significant antiviral activity, exhibiting EC50 values of 1 nM against HCV genotype 1a and 0.3 nM against genotype 1b. This compound is primarily utilized in research focused on HCV replication and the development of antiviral therapies. -
HCV NS5B Polymerase Inhibitor
MK3281 is a non-nucleoside inhibitor targeting the hepatitis C virus (HCV) NS5B polymerase. It demonstrates significant antiviral activity, with an EC50 of 28 nM for genotype 1a. This compound is utilized in research focused on antiviral drug development and understanding HCV replication mechanisms. -
NS5B Polymerase Inhibitor
PSI-353661 is a purine nucleotide inhibitor targeting the NS5B polymerase of Hepatitis C Virus (HCV). It demonstrates potent antiviral activity with EC90 values of 8 nM for wild-type HCV and 11 nM for the S282T resistant strain. Additionally, PSI-353661 achieves elevated levels of its active triphosphate form in primary human hepatocytes, making it a valuable tool for studying HCV replication and resistance mechanisms.
