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Catalog No.
Product Name
Application
Product Information
Citations
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nudix hydrolase family inhibitor
TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM). -
DNA replication inhibitor
Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. -
RAD51 inhibitor
Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain. -
DNA polymerase theta (Polθ) inhibitor
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ), with an IC50 of 5.8 nM as measured by the PicoGreen assay. It exhibits significant antitumor efficacy in mouse xenograft models. Additionally, RP-6685 contains an alkyne functional group, making it a useful click chemistry reagent capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, enabling its application in chemical biology and drug discovery research. -
DHX9 inhibitor
ATX968 (example 31) is an orally active, potent, and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 of 0.054 μM in circBRIP1-expressing models. It demonstrates robust and durable tumor growth inhibition or regression in mouse xenograft studies using microsatellite instability-high (MSI-H) and mismatch repair-deficient (dMMR) colorectal cancer cell lines, highlighting its potential for targeted cancer therapy. -
Polθ DNA polymerase inhibitor
ART899 is a highly specific allosteric inhibitor of the DNA polymerase domain of polymerase theta (Polθ). It effectively enhances the radiosensitivity of tumor cells and demonstrates good tolerability when combined with fractionated radiation therapy. ART899 significantly reduces tumor growth compared to radiation alone, making it a promising candidate for combination cancer radiotherapy strategies. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
POLRMT inhibitor
IMT1 is a first-in-class, specific, and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). It induces a conformational change in POLRMT, preventing substrate binding and inhibiting transcription in a dose-dependent manner in vitro. IMT1 decreases deoxynucleoside triphosphate levels and citric acid cycle intermediates, leading to significant depletion of cellular amino acid levels. IMT1 holds potential for the treatment of diseases associated with mitochondrial transcription disorders. -
WRN inhibitor
HRO761 (Werner syndrome RecQ helicase-IN-1, example 42) is a potent and selective inhibitor of the Werner syndrome RecQ DNA helicase (WRN), an essential enzyme involved in DNA replication, repair, and genome stability. Inhibition of WRN has shown synthetic lethality in cancers with microsatellite instability (MSI) or deficient DNA mismatch repair (dMMR), making HRO761 a promising candidate for targeted cancer therapy. It is being explored in preclinical cancer research to evaluate its efficacy in selectively killing WRN-dependent tumor cells while sparing normal cells. -
PolΘ inhibitor
PolQi2 is a selective inhibitor of DNA polymerase theta (Polθ), specifically targeting its N-terminal helicase domain to suppress the alternative end-joining (alt-EJ) DNA repair pathway. By inhibiting Polθ, PolQi2 enhances the precision and integration efficiency of CRISPR/Cas9-mediated gene editing across diverse genomic loci and cell lines. Furthermore, when used in combination with DNA-PK inhibitors, PolQi2 significantly reduces off-target effects associated with Cas9 activity. These properties make PolQi2 a valuable tool for improving the fidelity and efficiency of gene editing applications in both basic research and potential therapeutic contexts. -
RNA pol III inhibitor
ML-60218 is a broad-spectrum RNA polymerase III (Pol III) inhibitor with IC₅₀ values of 32 μM in *Saccharomyces cerevisiae* and 27 μM in human cells. It inhibits Pol III–mediated transcription, which is essential for the synthesis of small RNAs such as tRNAs and 5S rRNA. ML-60218 has been shown to disrupt pre-assembled viroplasms and prevent the formation of new ones, indicating its antiviral potential. Notably, this activity occurs independently of de novo transcription of host cellular RNAs, suggesting a direct effect on viral replication machinery. ML-60218 is a valuable tool for studying Pol III function and holds potential for antiviral research. -
POLRMT inhibitor
IMT1B (LDC203974) is an orally bioavailable, noncompetitive, and selective allosteric inhibitor of mitochondrial RNA polymerase (POLRMT). By targeting POLRMT, IMT1B disrupts mitochondrial DNA (mtDNA) transcription and impairs mitochondrial gene expression, leading to reduced mitochondrial function. This mechanism contributes to its potent anti-tumor effects, particularly in cancer cells that are highly dependent on mitochondrial metabolism. IMT1B holds promise as a therapeutic agent for targeting mitochondrial vulnerabilities in tumors. -
glutamine amidotransferase inhibitor
Azaserine (CI-337) is a glutamine analog and competitive inhibitor of glutamine amidotransferase, an enzyme involved in nucleotide biosynthesis. It exhibits both antibiotic and antitumor properties by disrupting glutamine-dependent metabolic processes essential for cell proliferation. Azaserine demonstrates antibacterial activity and has shown antitumor effects in various cancer models. However, it has also been reported to possess tumorigenic potential under certain conditions, warranting cautious evaluation. -
POLA1-HDAC11 Inhibitor
GEM144 is a potent and orally bioavailable dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It promotes p53 acetylation, induces p21 activation, and triggers G1/S cell cycle arrest followed by apoptosis. GEM144 exhibits significant antitumor efficacy in human orthotopic malignant pleural mesothelioma xenograft models, highlighting its potential as a targeted therapeutic agent for aggressive thoracic malignancies. -
POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
Pre-mRNA Splicing Inhibitor
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome. -
DNA Synthesis Inhibitor
Fludarabine triphosphate is a potent inhibitor of DNA synthesis, primarily targeting DNA primase. This nucleotide analog effectively inhibits DNA primase with an IC50 value of 2.3 μM and a Ki of 6.1 μM, obstructing the formation of primer RNA and ultimately disrupting DNA synthesis. Additionally, Fludarabine triphosphate also inhibits ribonucleotide reductase and DNA polymerase, leading to cellular apoptosis. It is utilized in various research applications to study mechanisms of DNA replication and the effects of nucleotide analogs on cell viability. -
DNA Synthesis Inhibitor
(rel)-Oxaliplatin is a DNA synthesis inhibitor that functions through the formation of DNA crosslinks, thereby obstructing DNA replication and transcription. This compound induces apoptosis in cancer cells, making it a valuable tool for studying cancer biology and treatment mechanisms. It is widely utilized in cancer research to explore therapeutic strategies targeting DNA repair pathways. -
DNA Synthesis Inhibitor
Sterigmatocystine is a DNA synthesis inhibitor that primarily targets the G1 phase of the cell cycle. As a mycotoxin produced by Aspergillus versicolor, it effectively inhibits p21 activity, leading to disruptions in cellular proliferation. Sterigmatocystine exhibits teratogenic and carcinogenic properties in animal models, making it a significant compound for studies in toxicology and cancer research. This reagent can facilitate investigations into the mechanisms of carcinogenesis and the effects of mycotoxins on cellular processes. -
mtDNA Synthesis Inhibitor
Alovudine (3'-Fluoro-3'-deoxythymidine) is an inhibitor of mitochondrial DNA (mtDNA) synthesis and serves as a marker for DNA synthesis. This compound demonstrates reduced susceptibility to inflammatory changes compared to traditional markers, making it a more reliable biomarker in pancreatic cancer studies. Additionally, Alovudine exhibits significant anti-orthopoxvirus and anti-leukemic activities, providing valuable insights for ongoing research in virology and oncology. -
DNA Synthesis Inhibitor
Cytarabine triphosphate trisodium is a competitive inhibitor of DNA synthesis, functioning as an active metabolite of Cytarabine. It is used primarily in research to assess the chemosensitivity of leukemic blasts to Cytarabine by measuring intracellular levels. This compound plays a critical role in studies related to leukemia treatment and the evaluation of drug efficacy in cancer therapies. -
RNA/DNA Synthesis Inhibitor
Sodium Camptothecin is a plant-derived alkaloid that functions primarily as an RNA and DNA synthesis inhibitor. It exhibits potent antitumor activity by effectively inhibiting the replication of adenoviruses, leading to significant disruption of viral DNA integrity. This compound is valuable for research applications focused on viral replication mechanisms and cancer therapy investigations. -
DNA/RNA Synthesis Inhibitor
DHPS-IN-1 is a potent inhibitor of dihydropteroate synthase (DHPS), exhibiting a remarkable inhibitory potency with an IC50 of 0.014 μM. This compound effectively impedes DNA and RNA synthesis, demonstrating significant anti-melanoma activity. DHPS-IN-1 is relevant for research applications focused on understanding metabolic pathways in cancer and developing targeted therapies against melanoma. -
DNA/RNA Synthesis Inhibitor
3-Isomangostin is a potent inhibitor of the MutT homologue 1 (MTH1) with an IC50 value of 52 nM, impacting DNA and RNA synthesis. Derived from the shell of Garcinia mangostana L., it presents a valuable chemical tool for investigating anticancer mechanisms and developing novel therapeutic strategies against cancer. Its ability to inhibit MTH1 highlights its potential for applications in cancer research and drug discovery. -
RNA Synthesis Inhibitor
Nitracrine is an RNA synthesis inhibitor that covalently and reversibly binds to DNA, forming covalent adducts in vivo. As a 1-nitroacridine derivative, it exhibits potent hypoxia-selective cytotoxicity in vitro and serves as an effective antitumor agent. Nitracrine demonstrates cytotoxic effects against a wide range of cell types, making it a valuable tool for cancer research and therapeutic investigations. -
DNA/RNA Synthesis Inhibitor
Methotrexate α-tert-butyl ester is an antimetabolite and antifolate compound that acts as a potent inhibitor of DNA and RNA synthesis. It demonstrates significant anti-tumor activity by effectively reducing tumor growth in HT1080 tumor-bearing mouse models. This compound is also utilized for its immunosuppressive and antineoplastic properties in various research applications. -
DNA Synthesis Inhibitor
Cytarabine triphosphate (Ara-CTP) is a competitive inhibitor of DNA synthesis, serving as an active metabolite of Cytarabine. This compound plays a crucial role in cellular mechanisms by disrupting normal DNA replication processes. Its intracellular levels are valuable for predicting the chemosensitivity of leukemic blasts to Cytarabine, making it a significant biomarker in the treatment of leukemia and related hematological disorders. -
DNA Synthesis Inhibitor
Cytembena is a potent inhibitor of DNA synthesis, primarily targeting replicative DNA processes, purine biosynthesis, and tetrahydrofolate formylase activity. Its biological activity demonstrates significant anti-cancer effects, particularly in the treatment of ovarian and breast cancer, as well as providing pain relief in cases of skeletal metastases. This compound is valuable in research applications focused on cancer therapeutics and the mechanisms of DNA replication and repair. -
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. -
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. -
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. -
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. -
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. -
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. -
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 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. -
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. -
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 Synthesis Inhibitor
Nitracrine hydrochloride is an RNA synthesis inhibitor that targets hypoxic cancer cells through its platinum-based structure. It demonstrates significant cytotoxicity against the Chinese hamster ovary cell line AA8 under low oxygen conditions, primarily by forming covalent adducts with DNA. This compound's mechanism involves reductive metabolism, leading to the formation of alkylating agents that enhance its reactivity with DNA. By inhibiting RNA synthesis, Nitracrine hydrochloride contributes to its overall anti-tumor efficacy, making it a valuable reagent for cancer research. -
DNA Synthesis Inhibitor
Methyl 3-oxodecanoate is a DNA synthesis inhibitor targeting protein synthesis at the level of translation initiation. This compound exhibits biological activity against human pathogens, including fluorescent haplophyllum and its culture supernatant. It serves as a valuable reagent for research applications focused on understanding virulence factors and mechanisms of DNA synthesis inhibition.
