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DNA Polymerase Inhibitor
Lucidenic lactone is a terpene compound that serves as an effective inhibitor of DNA polymerase. This compound demonstrates significant inhibitory activity against calf DNA polymerase-α (IC50 = 42 μM), rat DNA polymerase-β (IC50 = 99 μM), and HIV-1 reverse transcriptase (IC50 = 69 μM). Lucidenic lactone is valuable for research in molecular biology and virology, particularly in studies investigating DNA replication and reverse transcription processes. -
DNA Synthesis Terminator
3'-O-(2-Nitrobenzyl)-dATP is a photolabile DNA synthesis terminator that specifically targets the 3'-end of growing DNA strands. Its incorporation results in the cessation of DNA synthesis in a base-specific manner. Upon exposure to UV light, the 3'-protecting nitrobenzyl group is efficiently removed, allowing for the reinitiation of DNA synthesis. This compound is particularly valuable in the development of the Base Addition Sequencing Scheme (BASS), facilitating iterative stop-start cycles in DNA synthesis. -
Nucleoside Analogs
5'-Amino-5'-deoxyuridine is a nucleoside analog that serves as an important precursor for nucleic acid synthesis. It exhibits incorporation into DNA and RNA, allowing for the study of nucleic acid metabolism and function. This compound is widely utilized in molecular biology and genetic research applications, including the development of antiviral and anticancer therapies. -
DNA Polymerase α inhibitor
Aphidicolin 17-acetate is a selective inhibitor of eukaryotic DNA polymerase α. This compound significantly impairs in vivo DNA synthesis in model systems such as sea urchin embryos and HeLa cells while demonstrating no effect on RNA and protein synthesis. Its specificity for DNA polymerase α, without inhibition of polymerases β and γ, makes Aphidicolin 17-acetate a valuable tool for studying DNA replication processes and cellular responses to DNA damage. -
RNA polymerase Inhibitor
RNA polymerase-IN-2 is a potent inhibitor of DNA-dependent RNA polymerase, targeting the transcription processes in cells. This compound has been shown to effectively inhibit CYP isozymes, making it a valuable tool for studies investigating RNA synthesis and related metabolic pathways. Its applications extend to research in gene regulation and the development of potential therapeutic strategies targeting RNA polymerase activity. -
DNA/RNA Synthesis Inhibitor
Ledoxantrone trihydrochloride is a DNA/RNA synthesis inhibitor that targets DNA helicases, exhibiting an IC50 of 0.17 μM. This compound is primarily utilized in cancer research, particularly in studies related to prostate cancer, to explore its effects on cellular proliferation and gene expression pathways. -
HCMV DNA Polymerase Alpha Inhibitor
Naphthol AS-BS is a selective inhibitor of human cytomegalovirus (HCMV) DNA polymerase alpha, exhibiting an IC50 of 12 μM. This compound is significant for research into viral infections, particularly in understanding the mechanisms of HCMV replication and potential therapeutic interventions. Its inhibitory properties make it a valuable tool in virology studies and drug development efforts targeting HCMV. -
MTH1 Inhibitor
IACS-4759 is a potent and selective inhibitor of MTH1 (MutT homolog 1), with an IC50 value of 0.6 nM. This compound exhibits significant anti-cancer activity by disrupting the repair of damaged nucleotides, thereby inducing metabolic stress in cancer cells. IACS-4759 is useful for research applications focused on cancer metabolism and the development of targeted cancer therapies. -
HCV NS5B RNA-dependent RNA Polymerase Inhibitor
HCV-IN-50 is a potent inhibitor of HCV NS5B RNA-dependent RNA polymerase, demonstrating a selective competitive mechanism with an IC50 of 0.3 μM for the NS5B △C21 enzyme compared to the △C55 variant. This compound exhibits significant antiviral activity, effectively inhibiting the replication of Hepatitis C virus subgenomic replicons, including mutant strains. HCV-IN-50 is valuable for research applications focused on HCV replication mechanisms and antiviral drug development. -
Antibacterial Agent, RNA Polymerase Inhibitor
2,5-Di-tert-butyl-1,4-benzoquinone serves as a potent antibacterial agent and an effective RNA polymerase inhibitor. Isolated from the marine species Streptomyces sp. VITVSK1, this compound exhibits significant antibacterial activity, providing critical insights into combating emerging antibacterial resistance. Its ability to inhibit RNA polymerase further supports its value in research applications focused on microbial gene expression and antibiotic mechanisms. -
DNA Polymerases α/δ/ε Inhibitor
PMEG is an inhibitor of nuclear DNA polymerases α, δ, and ε, leading to DNA chain termination and suppression of DNA synthesis, which induces cytotoxicity in rapidly dividing cells. As an acyclic nucleotide phosphonate, PMEG is converted within cells to its active form, PMEG diphosphate. This compound demonstrates efficacy against leukemia and melanoma in rodent models and exhibits antiviral activity against various DNA viruses, including murine and human cytomegalovirus. PMEG serves as a valuable reagent for research into non-Hodgkin's lymphoma and related areas of study. -
DNA Alkylator
DGN549-L is a DNA alkylator that facilitates the alkylation of DNA, allowing for efficient conjugation to antibodies at lysine residues. This compound is particularly useful in the synthesis of antibody-drug conjugates (ADCs), enabling targeted delivery of therapeutic agents. Its application in bioconjugation research supports advancements in precision medicine and therapeutic development. -
TROP2 Directed Agent, Topoisomerase I Inhibitor
Sacituzumab tirumotecan is an antibody-drug conjugate that functions as a TROP2-directed agent and a topoisomerase I inhibitor. With a TROP2 EC50 of 2.787 ng/ml and a topoisomerase I IC50 of 0.7 μmol/L, it effectively delivers its cytotoxic payload to target cells. This compound is utilized in research focusing on metastatic triple-negative breast cancer and metastatic non-small cell lung cancer, making it crucial for studies aimed at understanding treatment mechanisms and therapeutic efficacy in these challenging malignancies. -
Topoisomerase Inhibitor
(4-NH2)-Exatecan is a topoisomerase inhibitor and a derivative of Exatecan. It exhibits significant biological activity by disrupting the DNA replication process, making it a valuable tool in cancer research. Additionally, (4-NH2)-Exatecan is suitable for the synthesis of antibody-drug conjugates (ADCs), facilitating targeted therapeutic applications in oncology. -
Topoisomerase I Inhibitor
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a topoisomerase I inhibitor that effectively interferes with DNA replication and transcription by stabilizing the DNA-enzyme complex. This compound demonstrates significant potential in antibody-drug conjugate (ADC) applications, showing efficient delivery to cells for targeted therapy. Its efficacy has been validated in both in vivo and in vitro models, making it a valuable tool for cancer research and therapeutic development. -
DNA Topoisomerase I Inhibitor
Ac-Exatecan is an acetylation-modified derivative of Exatecan, primarily functioning as an inhibitor of DNA Topoisomerase I, with an IC50 of 2.2 μM. This compound exhibits significant antitumor activity, making it a valuable payload for antibody-drug conjugate (ADC) applications. Ac-Exatecan is particularly effective against cells with P-glycoprotein-mediated multidrug resistance, offering potential in overcoming therapeutic challenges associated with resistant tumor types. -
DNA topoisomerase I Inhibitor
(αR)-Cyclopropaneacetamide-Exatecan is a potent inhibitor of DNA topoisomerase I, exhibiting enhanced membrane permeability with an IC50 value of 1.34 μM against the human enzyme. This compound induces cytotoxicity through the suppression of topoisomerase I activity, displaying anticancer effects that are independent of HER2 expression levels. Derived from Exatecan, (αR)-Cyclopropaneacetamide-Exatecan serves as an antibody-drug conjugate cytotoxin and is applicable in research on various advanced cancers, including breast, gastric, colorectal, and non-small cell lung cancers. -
Topoisomerase Inhibitor
Mal-Exatecan is a maleimide-modified derivative of Exatecan, acting primarily as a DNA topoisomerase I inhibitor. This compound demonstrates potent antitumor activity by stabilizing the topoisomerase-DNA complex, leading to DNA strand breaks and subsequent cell death in rapidly dividing cancer cells. Mal-Exatecan is primarily utilized in cancer research to explore therapeutic strategies targeting topoisomerase I. -
DNA topoisomerase I Inhibitor
DRF-1042 is a potent inhibitor of DNA topoisomerase I, derived from Camptothecin. It demonstrates significant anticancer activity against a diverse range of human cancer cell lines, including those exhibiting multi-drug resistance (MDR). This compound is valuable for research applications focused on cancer therapeutics and the mechanisms of resistance in tumor cells. -
Topoisomerase I Inhibitor
Exatecan mesylate dihydrate is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 of 2.2 μM (0.975 μg/mL). This compound is particularly relevant in cancer research, as it interferes with DNA relaxation during replication, subsequently leading to apoptosis in rapidly dividing cells. Its application extends to various studies focused on chemotherapeutic mechanisms and the development of novel anti-cancer therapies. -
DNA topoisomerase I Inhibitor
Rebeccamycin is a potent inhibitor of DNA topoisomerase I, a key enzyme involved in DNA replication and transcription. This antitumor antibiotic primarily exerts its cytotoxic effects by stabilizing the topoisomerase I-DNA cleavage complex, leading to DNA damage and apoptosis in cancer cells. Rebeccamycin shows minimal activity against protein kinase C and topoisomerase II, making it a selective agent for research in cancer biology and therapeutic development. -
Topoisomerase I Inhibitor
Exatecan hydrochloride is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 value of 2.2 μM (0.975 μg/mL). This compound is primarily utilized in cancer research, facilitating investigations into the mechanisms of tumor cell proliferation and survival by disrupting the topological state of DNA during replication. Its activity makes it a valuable tool for exploring therapeutic options and treatment strategies in oncology. -
Topoisomerase I Inhibitor
Exatecan analog 38 is a potent topoisomerase I inhibitor derived from camptothecin. This compound exhibits significant cytotoxicity against various cancer cell lines, making it a valuable tool for oncology research. Exatecan analog 38 can be utilized in the development of antibody-drug conjugates (ADCs) by conjugating it to monoclonal antibodies through linkers, enhancing targeted therapeutic applications. -
Topoisomerase I Inhibitor
LD2-3 is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound can be conjugated to monoclonal antibodies via linkers to create antibody-drug conjugates (ADCs), facilitating targeted therapy applications. LD2-3 is particularly suited for use in studies involving carcinoembryonic antigen (CEA) overexpressing tumors, enabling researchers to explore its efficacy in a precision oncology context. -
eIF4A Inhibitor
eIF4A-IN-2 is a potent inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound demonstrates significant cytotoxic activity and can be utilized as a valuable payload in the synthesis of antibody-drug conjugates (ADCs). Researchers investigating translation regulation and therapeutic strategies in cancer may find eIF4A-IN-2 particularly useful for advancing their studies. -
DNA Topoisomerase Inhibitor
(5-Cl)-Exatecan is a potent inhibitor of DNA topoisomerase, primarily utilized in cancer research settings. This compound functions as an antibody-drug conjugate (ADC) cytotoxin, targeting and disrupting the DNA replication process in cancer cells. Its efficacy in selectively inducing cytotoxicity makes it a valuable tool for studying cancer therapeutics and exploring the mechanisms of drug resistance. -
Telomerase Inhibitor
L2H2-6OTD is a potent telomerase inhibitor that functions through G-quadruplex stabilization. This compound demonstrates significant telomerase inhibitory activity with an IC50 value of 15 nM, making it a valuable tool in cancer research. It can be utilized to investigate telomere biology, the mechanisms underlying cellular aging, and potential therapeutic strategies targeting telomerase in cancer cells. -
Topoisomerase Inhibitor
MC-DOXHZN (hydrochloride) is a topoisomerase II inhibitor that serves as an albumin-binding proagent of Doxorubicin. This compound features acid-sensitive properties, enabling it to selectively release Doxorubicin in tumor microenvironments. MC-DOXHZN is particularly valuable for antibody-drug conjugate (ADC) synthesis, facilitating targeted cancer therapies. Its unique mechanism enhances the potential for effective treatment strategies in oncology research. -
EIF2α Activator
HR-19011 is an eIF2α phosphorylation activator that specifically targets the heme-regulated inhibitor HRI (EIF2AK1). It demonstrates significant growth inhibitory activity against K562 leukemia cells, with an IC50 value of 3.91 µM. By activating the integrated stress response through the HRI-eIF2α-ATF4 axis, HR-19011 effectively contributes to the suppression of hematologic malignancies. Its favorable safety profile in vivo further supports its use in research focused on leukemia and other blood-related cancers. -
Fluorescence Dye
Cy5 maleimide is a cyanine-based fluorescent dye that covalently binds to thiol groups in proteins and other biomolecules. Characterized by its long wavelength emission, high extinction coefficient, and excellent water solubility, Cy5 maleimide is ideal for applications in fluorescence microscopy, flow cytometry, and other labeling techniques. The straightforward mixing reaction facilitates efficient labeling of proteins and antibodies, making it a valuable tool for various biological research applications, including immunoassays and in vivo imaging studies. -
Fluorescent Dye
CY5-N3 (Sulfo-Cyanine5-azide) is a cell-permeable fluorescent dye, with excitation and emission wavelengths of 646 nm and 662 nm, respectively. This compound is designed for use in live cell imaging applications, enabling visualization of cellular processes in real time. CY5-N3 can be utilized effectively in Click chemistry reactions for conjugating with various biomolecules, facilitating enhanced imaging strategies in biological research. -
HDAC1 Inhibitor, NTR/pH Fluorescence Inducer
HDAC-IN-101 is a selective inhibitor of HDAC1, exhibiting an IC50 of 65 nM against human HDAC1. This compound effectively inhibits cancer cell proliferation by targeting HDAC1 activity. In addition, HDAC-IN-101 is metabolically activated by overexpressed nitroreductase to produce H6AQ, which displays fluorescence under low pH conditions. Its unique properties make it valuable for applications in cancer research and cellular imaging studies. -
Topoisomerase II Inhibitor
Amrubicin hydrochloride is a potent inhibitor of DNA topoisomerase II, a key enzyme involved in DNA replication and repair. This compound exhibits significant antitumor activity and has been studied for its efficacy in various cancer models. It is utilized in research to explore mechanisms of action in chemotherapy and to evaluate potential therapeutic strategies against tumors. -
Type IIA Topoisomerases Inhibitor
GSK945237 is a potent inhibitor of bacterial type IIA topoisomerases, exhibiting strong bactericidal activity. It demonstrates broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria, with an IC50 of 0.034 μg/mL against Helicobacter influenzae DNA gyrase. In vivo studies indicate significant effectiveness in a rat model of respiratory tract infection, highlighting its potential applications in anti-infection research. -
Topoisomerase II Inhibitor
CP-67015 is a potent topoisomerase II inhibitor that exhibits direct mutagenic effects in mammalian cells, impacting both gene and chromosomal levels. As a quinolone antibiotic, it demonstrates significant biological activity, making it a valuable tool for researchers investigating DNA manipulation and repair mechanisms. CP-67015 is suitable for studies focused on the role of topoisomerase II in cellular processes and the effects of targeted DNA damage. -
DNA Gyrase/Topoisomerase Inhibitor
Levofloxacin mesylate is a potent DNA gyrase and topoisomerase IV inhibitor. As an orally active antibiotic, it exhibits significant antibacterial activity against both Gram-positive and Gram-negative bacteria. This compound is applicable in various research contexts, including studies on chronic periodontitis, airway inflammation, and BK viremia. Additionally, levofloxacin mesylate demonstrates anti-orthopoxvirus properties, making it valuable for investigations into viral infections. -
Topoisomerase Inhibitor
OSUAB-0284 is a potent bacterial topoisomerase inhibitor, exhibiting significant anti-staphylococcal activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA). By targeting and inhibiting bacterial topoisomerase, OSUAB-0284 effectively disrupts bacterial DNA replication and transcription processes. This compound is valuable for researching infections linked to drug-resistant bacteria, providing insights into potential therapeutic strategies against MRSA and other related pathogens. -
Topoisomerase Inhibitor
(1R,2S,7R)-Sitafloxacin is a potent inhibitor of topoisomerases, specifically targeting DNA gyrase with an IC50 of 0.18 μg/mL. This stereoisomer's activity highlights its potential in elucidating the role of topoisomerase-mediated DNA manipulation in various biological processes. It serves as a valuable tool in molecular and cellular research applications focusing on DNA replication and repair mechanisms. -
Nucleoside Analog
Galocitabine is a nucleoside analog that functions primarily by inhibiting nucleic acid synthesis, leading to the suppression of cancer cell proliferation and antiviral activity. This compound exhibits notable efficacy against various cancer types and can be utilized in research focused on exploring therapeutic strategies for oncological and viral diseases. Its mechanism makes it a valuable tool in studying cellular responses and treatment pathways in cancer biology and virology. -
ATR Inhibitor
ATR-IN-31 is a selective ATR kinase inhibitor that exhibits an IC50 of 7 nM, demonstrating its potent activity. This compound functions by specifically inhibiting ATR kinase activity without significantly affecting ATM kinase. ATR-IN-31 has shown efficacy in reducing the viability of prostate cancer cells, making it a valuable tool for research focused on prostate cancer. -
ATM/ DNA-PKcs Inhibitor
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms. -
ATR Substrate
ATR kinase substrate peptide (ASELPASQPQPFSAKKK) functions as a specific substrate for ATR protein kinase, facilitating the detection of ATR kinase activity in biological research. This peptide is instrumental in studying cellular responses to DNA damage and the associated signaling pathways. It plays a critical role in validating ATR kinase activity and exploring its implications in cancer biology and therapeutic development. -
ATR Inhibitor
(S)-Ceralasertib is an ATR inhibitor, specifically targeting ataxia telangiectasia mutated and rad3 related (ATR) signaling pathways. This compound exhibits significant potential in cancer research by enhancing the sensitivity of tumor cells to DNA-damaging agents through inhibition of the ATR pathway. (S)-Ceralasertib is utilized in studies aimed at understanding the roles of DNA repair mechanisms and evaluating combination therapies for various cancers. -
ATM Inhibitor
WSD0628 is a potent ATM inhibitor known for its ability to cross the blood-brain barrier. It exhibits significant radiosensitizing effects, making it a valuable tool for research in cancer therapy and radiobiology. Its inhibition of the ATM pathway has implications for enhancing the efficacy of radiotherapy in various malignancies. -
PROTAC ATR Degrader
PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies. -
ATM Inhibitor
M3541 is a potent, ATP-competitive inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 0.25 nM. This compound demonstrates significant selectivity against other protein kinases. M3541 effectively hinders the repair of double-strand breaks (DSB) and displays notable antitumor activity, making it a valuable tool for cancer research and therapeutic studies targeting DNA damage response pathways. -
ATM/ATR
SKLB-197 is a selective inhibitor of ATR (ATM and Rad3-related protein) with an IC50 value of 0.013 μM, demonstrating minimal activity against a panel of 402 other protein kinases. This compound exhibits significant antitumor efficacy specifically in ATM-deficient tumors, showing potent activity in both in vitro and in vivo models. SKLB-197 serves as a valuable tool for investigating the roles of ATM and ATR in cancer biology and for the development of targeted therapies. -
ATR Inhibitor
ATR-IN-4 is a selective inhibitor of the ATR (Ataxia Telangiectasia Mutated and Rad3-related) kinase. This compound exhibits significant antiproliferative activity against human prostate cancer cells (DU145) and human lung cancer cells (NCI-H460), yielding IC50 values of 130.9 nM and 41.33 nM, respectively. ATR-IN-4 is valuable for research investigating DNA damage response pathways and potential therapeutic strategies in cancer treatment. -
Atm Inhibitor
ATM Inhibitor-10 is a selective ATM inhibitor characterized as a 3-quinoline carboxamide with an IC50 of 0.6 nM. This compound demonstrates significant anti-tumor activity in SW620 xenograft models and shows synergistic effects when combined with Top I inhibitors. It serves as a valuable tool for studies involving DNA damage response and cancer therapeutics. -
PROTAC ATR Degrader
Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage.

