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Catalog No.
Product Name
Application
Product Information
Citations
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HDAC Inhibitor, Topoisomerase I Inhibitor
WJ35435 is a dual-target HDAC and topoisomerase I inhibitor that exerts anticancer activity by inducing DNA damage and promoting cell cycle arrest at the G1 and G2 phases, ultimately leading to apoptosis. This compound enhances histone H3 acetylation and phosphorylation, along with α-tubulin acetylation and the formation of γ-H2AX, thereby effectively demonstrating its anti-HDAC properties. WJ35435 holds potential for advancing research in cancer therapeutics. -
PARP1 Inhibitor
KU-0058948 hydrochloride is a highly selective inhibitor of PARP1, exhibiting an IC50 of 3.4 nM. It is demonstrated to induce cell cycle arrest and apoptosis in primary myeloid leukemic cells and various myeloid leukemic cell lines. This reagent is valuable for research into the mechanisms of leukemia and the therapeutic potential of PARP inhibition in hematological malignancies. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 10 is a potent inhibitor of the topoisomerase II enzyme, exhibiting an IC50 value of 7.45 µM. This compound effectively induces cell cycle arrest in the G2-M phase and promotes apoptosis in HepG-2 cells. Additionally, Topoisomerase II inhibitor 10 demonstrates significant anti-proliferative activity against various cancer cell lines, including HepG-2, MCF-7, and HCT-116, making it a valuable tool for cancer research applications. -
HDAC Inhibitor
HDAC-IN-46 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.21 μM for HDAC1 and 0.021 μM for HDAC6. In MDA-MB-231 cells, HDAC-IN-46 promotes the upregulation of phosphorylated p38 while downregulating Bcl-xL and cyclin D1, leading to significant G2 phase cell cycle arrest and apoptosis. This compound is valuable for research focused on triple-negative breast cancer (TNBC). -
PARP1/NAMPT Inhibitor
PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research on triple-negative breast cancer (TNBC). -
HDAC Inhibitor
HDAC-IN-57 is a potent orally active inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 2.07 nM for HDAC1, 4.71 nM for HDAC2, 2.4 nM for HDAC6, and 107 nM for HDAC8. In addition, HDAC-IN-57 inhibits lysine-specific demethylase 1 (LSD1) with an IC50 of 1.34 µM. This compound induces apoptosis and demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development targeting epigenetic regulation. -
PARP1/c-Met Inhibitor
PARP1/c-Met-IN-1 is a selective dual inhibitor targeting PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest in the G2/M phase in MDA-MB-231 cells. Additionally, PARP1/c-Met-IN-1 has shown significant antitumor activity in murine models, making it a valuable tool for cancer research and therapeutic development. -
PARP1 Inhibitor
PARP1-IN-10 is a potent inhibitor of PARP1, exhibiting an IC50 value of 50.62 nM in vitro without inducing cytotoxic effects. This compound induces cell cycle arrest at the G2/M phase and promotes apoptosis, thereby enhancing the cytotoxic efficacy of temozolomide (TMZ). PARP1-IN-10 is valuable for research in cancer biology and therapeutics, particularly in understanding the interplay between DNA repair mechanisms and chemotherapeutic sensitivity. -
PARP1 Inhibitor
PARP1-IN-55 is a selective inhibitor of PARP1, demonstrating potent activity with an IC50 of 0.019 μM. It exhibits considerable anti-proliferative effects on MCF-7 breast cancer cells, with an IC50 of 3.6 μM. By inhibiting the PARP1-mediated DNA damage repair pathway, PARP1-IN-55 induces reactive oxygen species accumulation, disrupts mitochondrial membrane potential, and promotes apoptosis while inhibiting cancer cell migration, invasion, and colony formation. This compound serves as a valuable tool for investigating breast cancer biology and therapeutic strategies. -
Poly (ADP-ribose) Polymerase Inhibitor
8-NH2-ATP is an inhibitor of poly (ADP-ribose) polymerase (PARP), acting as a critical tool in research on cell apoptosis. This compound is derived from 8-NH2-Ado and exhibits potent effects by inducing apoptotic cleavage of PARP, making it useful for studying mechanisms of cell death, DNA repair, and cancer therapeutics. Its applications extend to exploring PARP's role in various biological pathways and assessing the therapeutic potential of PARP inhibition in disease models. -
T4 DNA Polymerase Inhibitor
3'-Fluorothymidine-5'-triphosphate tetrasodium is a competitive inhibitor of T4 DNA polymerase, functioning as an analog of dTTP. By inhibiting T4 DNA polymerases, including wild-type, L98, and CB121 variants, it effectively disrupts DNA synthesis processes. This compound is valuable for research applications involving DNA replication studies and exploration of polymerase inhibition mechanisms. -
DNA polymerase θ Inhibitor
RTx-303 is a selective inhibitor of DNA polymerase θ (Polθ), with an IC50 value of 5.1 nM. This compound demonstrates potent cellular activity and enhances the efficacy of PARP inhibitors in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 is utilized in research focused on BRCA2-mutated breast cancer, providing valuable insights into therapeutic strategies targeting DNA repair mechanisms. -
HCV Polymerase Inhibitor
Dasabuvir sodium is a non-nucleoside inhibitor of hepatitis C virus (HCV) polymerase, specifically targeting the RNA-dependent RNA polymerase encoded by the HCV NS5B gene. It demonstrates potent antiviral activity against HCV genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC50 values of 7.7 nM and 1.8 nM, respectively. Dasabuvir sodium is primarily utilized in research focused on HCV replication and the development of antiviral therapies. -
DNA Gyrase/Topoisomerase Inhibitor
Levofloxacin sodium is a potent DNA gyrase and topoisomerase IV inhibitor that exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. Its primary applications include research on chronic periodontitis, airway inflammation, and BK viremia. Additionally, Levofloxacin sodium demonstrates anti-orthopoxvirus properties, making it a valuable reagent for studies involving viral infections. -
RNA Polymerase Activities Inhibitor
Thio-ITP (6-Thioinosine 5'-triphosphate) is a competitive inhibitor of RNA polymerase activities. It exhibits a high apparent affinity for RNA polymerases, with inhibition constants of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II. Thio-ITP is useful in research applications aimed at understanding transcriptional regulation and dissection of RNA polymerase mechanisms. -
MTH1 Inhibitor
MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), a target implicated in cancer biology. This compound exhibits significant anti-tumor activity, making it a valuable tool for cancer research. MTH1-IN-2 can be utilized to investigate the mechanisms of tumorigenesis and to develop therapeutic strategies that exploit the MTH1 pathway. -
DNA/RNA Synthesis Inhibitor
Riddelline is a pyrrolizidine alkaloid that functions as a potent inhibitor of DNA and RNA synthesis. It exhibits significant genotoxic properties by inducing elevations in unscheduled DNA synthesis and S-phase synthesis in rat liver models. This compound is utilized in research to study the mechanisms of genotoxicity and its implications in cellular processes and carcinogenesis. -
Topoisomerase I Inhibitor.
T-2513 hydrochloride is a selective inhibitor of topoisomerase I. By covalently binding to and stabilizing the topoisomerase I-DNA complex, it effectively inhibits DNA replication and RNA synthesis, resulting in cytotoxicity. This compound is utilized in research applications focused on cancer biology and the mechanisms of chemotherapeutic agents. -
RNA polymerase II Inhibitor
Dideoxy-amanitin is an allosteric inhibitor of RNA polymerase II, demonstrating potent selectivity with an IC50 of 74.2 nM. This compound is particularly valuable for research applications focused on transcriptional regulation and RNA synthesis inhibition. Its ability to selectively hinder RNA polymerase II makes it a crucial tool for investigating gene expression and related pathways in various biological contexts. -
DNA/RNA Synthesis Inhibitor
Bromochloroacetonitrile, a potent DNA/RNA synthesis inhibitor, exhibits direct mutagenic activity and can induce DNA strand breakage. This compound serves as a valuable tool in research focused on understanding DNA damage mechanisms and the effects of mutagens on genetic material. Its ability to disrupt nucleic acid synthesis makes it relevant for studies in genotoxicity and cancer research. -
Topoisomerase II Inhibitor
NK-611 is a topoisomerase II inhibitor that functions as an epipodophyllotoxin derivative. By inhibiting topoisomerase II with an IC50 of 56 μM, NK-611 induces DNA double-strand breaks, leading to effective antitumor activity. Unlike its parent compound Podofilox, NK-611 does not interfere with microtubule polymerization, thus minimizing associated side effects. This compound has shown potent efficacy in in vivo leukemia models and is valuable for cancer research applications. -
HBV DNA Synthesis Inhibitor
LB80317 is an active metabolite of LB80380 that functions as a potent inhibitor of HBV DNA synthesis, exhibiting an EC50 of 0.5 μM. This compound demonstrates antiviral activity, making it a promising candidate for the treatment of chronic hepatitis B. Its ability to inhibit viral replication supports its potential utility in HBV research and therapeutic applications. -
Topoisomerase I Inhibitor
T-2513 is a selective inhibitor of topoisomerase I, a critical enzyme involved in the relaxation of DNA supercoils during replication and transcription. By covalently binding to and stabilizing the topoisomerase I-DNA complex, T-2513 effectively inhibits DNA replication and RNA synthesis. This activity may induce cytotoxic effects, making it a valuable tool in cancer research and studies focused on cell proliferation and death. -
DNA Synthesis Inhibitor
Alldimycin A is an anthracycline compound that functions as a potent inhibitor of DNA and RNA synthesis. It demonstrates significant anti-proliferative activity against murine leukemic L1210 cells, exhibiting IC50 values of 0.05 μg/mL for growth inhibition, 0.92 μg/mL for RNA synthesis, and 0.47 μg/mL for DNA synthesis. Alldimycin A is valuable for research applications in cancer biology and the study of nucleic acid metabolism. -
DNA/RNA Synthesis Inhibitor
Ulicyclamide is a cytotoxic cyclic peptide that functions as a DNA and RNA synthesis inhibitor. Isolated from the tunicate Lissoclinum patella, Ulicyclamide effectively inhibits nucleic acid synthesis in leukemia cells. This compound is primarily utilized in research focused on leukemia and the underlying mechanisms of nucleic acid metabolism in cancer biology. -
DNA Synthesis Inhibitor
Teloxantrone is a potent DNA synthesis inhibitor with an IC50 of 0.33 μM. This compound exhibits significant antitumor activity and is particularly relevant in the study of colorectal cancer. Its ability to interfere with DNA replication makes it a valuable tool for cancer research and therapeutic investigations. -
RNA Polymerase Inhibitor
2'-Deoxy-2'-fluoro-l-uridine is an L-nucleoside that serves as a selective inhibitor of viral RNA polymerase. It effectively inhibits the replication of RNA viruses, making it a valuable tool for research focused on viral replication mechanisms and the development of antiviral therapies. This compound is instrumental for studies investigating RNA virus pathogenesis and potential therapeutic interventions. -
DNA/RNA Synthesis Inhibitor
Ledoxantrone is a potent inhibitor of DNA and RNA synthesis, specifically targeting DNA helicases with an IC50 of 0.17 μM. This compound demonstrates significant biological activity against cancer cells and is utilized in research focusing on prostate cancer. Its mechanism of action provides valuable insights into the role of DNA repair and replication in oncogenesis. -
Topoisomerase II Inhibitor
F-14512 hydrochloride is a potent inhibitor of topoisomerase II, functioning through the polyamine transport system (PTS) to selectively target cancer cells. By enhancing the binding affinity of polyamines to DNA, it effectively inhibits topoisomerase II activity, leading to significant cytotoxic effects in cells with elevated PTS activity and resulting in DNA damage. Additionally, F-14512 hydrochloride exhibits strong antitumor efficacy in the MX1 breast tumor xenograft model, making it a valuable reagent for cancer research, particularly in studies focusing on breast cancer. -
RNA Polymerase II Inhibitor
ε-Amanitin is a cyclic peptide that specifically inhibits RNA polymerase II activity by binding to the enzyme's active site. This potent inhibitor disrupts transcription elongation, making it a valuable tool for investigating gene expression mechanisms. ε-Amanitin is commonly utilized in research focused on transcription regulation, RNA processing, and studying the effects of transcriptional inhibition in various biological systems. -
DNA Synthesis/HSV/HIV-1 Inhibitor
16,16-Dimethyl prostaglandin A1 is a prostaglandin analog that primarily inhibits DNA synthesis. It demonstrates significant antiviral activity by reducing viral replication in both herpes simplex virus (HSV) and HIV-1 infection models. This compound serves as a valuable tool for research focused on cancer biology and viral pathogenesis. -
DNA Polymerase Inhibitor
ddhCTP is a nucleoside analog that acts as a selective inhibitor of DNA polymerase. It effectively disrupts DNA synthesis with Ki values of 1.32 μM for DNA polymerase beta and 0.034 μM for DNA polymerase gamma. This compound is valuable for research applications involving the study of DNA replication and polymerase-specific pathways, providing insights into cellular mechanisms and potential therapeutic targets. -
MTH1 Inhibitor
IACS-4619 is a highly selective inhibitor of the MTH1 enzyme (MutT homolog 1) with an IC50 of 0.2 nM. This 2-aminopyrimidine compound effectively blocks the hydrolysis of oxidized purine nucleotides, such as 8-oxo-dGTP, preventing the incorporation of these nucleotides into DNA. Notably, IACS-4619 demonstrates significant inhibition of endogenous MTH1 activity in MTH1-overexpressing U2OS cells without exhibiting antiproliferative or cytotoxic effects on various human cancer and normal cell lines. This reagent is applicable in oncology research targeting the MTH1 pathway. -
rRNA Synthesis Inhibitor
NusB-IN-1 is a potent inhibitor of bacterial rRNA synthesis, demonstrating significant antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Staphylococcus aureus (VRSA). This compound serves as a valuable tool in microbiological research and drug development targeting bacterial RNA synthesis mechanisms. Additionally, NusB-IN-1 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions, facilitating its use in click chemistry applications. -
DNA topoisomerase II Inhibitor
NSC 660028 is a potent inhibitor of DNA topoisomerase II, exhibiting an ID50 of 50 μM. This compound disrupts DNA topoisomerase II activity, leading to the induction of protein-linked DNA breaks. NSC 660028 is primarily utilized in cancer research to explore mechanisms of tumor cell proliferation and resistance. -
Dual MTH1/OGG1 Inhibitor
SU0383 is a dual inhibitor of MTH1 and OGG1, demonstrating IC50 values of 0.034 μM and 0.49 μM, respectively. This compound induces cytotoxicity in cancer cells and enhances their sensitivity to oxidative stress, while exhibiting minimal toxicity in normal cells. SU0383 is suitable for applications in cancer research, particularly in studies focused on oxidative stress responses and therapeutic strategies targeting DNA repair mechanisms. -
EV71 3D Polymerase Inhibitor
DTriP-22 is a potent inhibitor of the enterovirus 71 (EV71) 3D polymerase, characterized by low toxicity. It demonstrates broad-spectrum antiviral activity against RNA viruses, particularly within the picornavirus family, while exhibiting no effects on DNA viruses. By targeting and inhibiting viral RNA synthesis during the early stages of replication, DTriP-22 serves as a valuable reagent in anti-enterovirus research applications. -
DNA Polymerase λ Inhibitor
Procaspase-IN-5 is a selective inhibitor of human DNA polymerase λ, with significant implications for cancer research. It exhibits a potent inhibitory effect on DNA polymerization and terminal deoxynucleotidyl transferase (TdT) activities, with IC50 values of 5.9 μM and 4.5 μM, respectively. This compound serves as a valuable tool for studying the mechanisms of DNA replication and repair in cancer cells. -
Topoisomerase II Inhibitor
KW-2170 hydrochloride is a potent topoisomerase II inhibitor that functions by stabilizing the topoisomerase II-DNA complex. This stabilization leads to DNA double-strand breaks, thereby inhibiting DNA replication and transcription, which ultimately results in tumor cell death. KW-2170 hydrochloride demonstrates broad-spectrum anti-tumor activity in various mouse and human tumor models, making it a valuable reagent for research related to solid tumors. -
DNA Synthesis Inhibitor
7U85 is a potent DNA synthesis inhibitor that targets the processes involved in DNA replication. Its primary mechanism disrupts nucleotide incorporation, thereby impeding cell proliferation. This compound demonstrates significant potential for research applications in breast cancer studies, offering insights into tumor growth and treatment resistance mechanisms. -
DNA Synthesis Inhibitor
Miboplatin (DWA-2114R) is a platinum-based compound that functions as a DNA synthesis inhibitor. It effectively diminishes the template activity of both prokaryotic and eukaryotic DNA polymerases, making it valuable for research focused on DNA replication processes. This compound is useful in studies exploring DNA damage response, cancer biology, and potential therapeutic applications in oncology. -
Topoisomerase Inhibitor
NSC 727357 is a potent topoisomerase inhibitor and DNA intercalator, exhibiting significant antitumor activity. It effectively inhibits cell proliferation and induces G1 phase cell cycle arrest. This compound is particularly relevant for cancer research, including studies focused on melanoma. -
NS5B Polymerase Inhibitor
A-837093 sodium is a potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase, exhibiting high selectivity and oral bioavailability. It demonstrates strong inhibitory activity against HCV genotypes 1a (IC50 = 1.25 nM) and 1b (IC50 = 0.33 nM). A-837093 sodium has shown antiviral efficacy in in vivo studies involving HCV-infected chimpanzees, making it a valuable tool for research focused on HCV infection and therapeutic development. -
RNA Synthesis Inhibitor
Nitracrine dihydrochloride hydrate is an RNA synthesis inhibitor that covalently and reversibly binds to DNA, forming covalent adducts within biological systems. This 1-nitroacridine derivative exhibits potent hypoxia-selective activity in vitro and serves as an effective antitumor agent. Its cytotoxic properties extend to a wide range of cell types, making it a valuable compound for cancer research and studies focusing on DNA-targeting agents. -
DNA/RNA Synthesis Inhibitor
Ara-ATP is a structural analog of ATP that functions as an inhibitor of poly(A) polymerase activity through competitive interaction with ATP. This inhibition disrupts the biosynthesis of RNA, making Ara-ATP valuable for studies on RNA processing and regulation. It is particularly useful in examining mechanisms of gene expression and RNA metabolism in various cellular contexts. -
MTH1 aTAG inhibitor
MTH1 degrader-1 is a potent degrader targeting MTH1 through a PROTAC mechanism. This compound facilitates the selective degradation of MTH1, making it a valuable tool for studying the role of MTH1 in cancer metabolism and therapy resistance. Key applications include the development of PROTACs and the synthesis of related compounds, such as PROTAC aTAG 4531. -
Topoisomerase Inhibitor
Netropsin is a small-molecule minor-groove binder that functions as a topoisomerase inhibitor. It effectively inhibits the catalytic activity of isolated topoisomerase, disrupting the stabilization of cleavable complexes associated with both topoisomerase I and II. Additionally, Netropsin exhibits antibacterial and antiviral properties, making it a valuable tool for research in the fields of microbiology and virology. -
DNA Synthesis Inhibitor
2-Keto-D-galactose, also known as D-Galactosone, functions as a potent inhibitor of DNA synthesis. It displays significant biological activity by inhibiting the proliferation of Ehrlich ascites tumor cells in vitro, making it a valuable reagent for cancer research and studies involving cell growth regulation. This compound can be utilized to investigate the mechanisms of DNA synthesis disruption and its effects on tumor cell dynamics. -
RNA Polymerase Inhibitor
Adafosbuvir is a uridine-based nucleotide analog that serves as a potent RNA polymerase inhibitor targeting the NS5B protein of Hepatitis C virus (HCV). It exhibits significant antiviral activity by effectively inhibiting HCV replication. This compound is primarily utilized in research applications aimed at understanding HCV biology and developing antiviral therapies. -
Polθ Polymerase Inhibitor
Polθ-IN-9 is a selective inhibitor of Pol θ polymerase, demonstrating an IC50 value of 9.6 nM and a Kd of 47.5 nM, with no significant inhibitory effects on other human DNA polymerases such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. This compound exhibits potent antiproliferative activity in DLD1 BRCA2 knockout cells (IC50 = 2.9 μM) and MDA-MB-436 cells (IC50 = 4.9 μM), while also increasing DNA damage and γH2AX levels. In addition, Polθ-IN-9 has shown to inhibit tumor growth in conjunction with Olaparib in the MDA-MB-436 xenograft model, making it a valuable tool for studying homologous recombination-deficient cancers, including breast cancer.
