Catalog No.
Product Name
Application
Product Information
Citations
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RdRp inhibitor
Galidesivir hydrochloride (BCX 4430 hydrochloride) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile. -
DNA synthesis inhibitor
Thiarabine (OSI-7836) shows potent anti-tumor activity and inhibition of DNA synthesis. - NKP-1339 (IT-139) is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer with limited side effects.
- Zin Zin Ei, .et al. , Sci Rep, 2021, Nov 17;11(1):22448 PMID: 34789798
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radiosensitizer
3-AP (PAN-811) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer. -
signal transducing G proteins activator
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA. -
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. - Riamilovir, also known as Triazavirin, is a nucleoside analogue of nucleic acid and an antiviral agent, works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture.
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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. - L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
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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. -
DNA Repair/Replicase Modulator
N-Nitrosodiethylamine (Diethylnitrosamine, DEN) is a highly potent hepatocarcinogenic dialkylnitrosamine found in tobacco smoke, water, cheddar cheese, cured and fried foods, and various alcoholic beverages. It induces alterations in nuclear enzymes involved in DNA repair and replication, contributing to its carcinogenicity. DEN causes tumors across multiple animal species, primarily affecting the nasal cavity, trachea, lung, esophagus, and liver. -
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. -
RNA RIBOTAC Degrader
Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology. -
DNA Stain
7-Aminoactinomycin D (7-AAD) is a cell-impermeant fluorescent DNA stain that primarily targets and binds to GC-rich regions of DNA. This compound is often utilized in flow cytometry and fluorescence microscopy to assess cell viability and apoptosis. Additionally, 7-AAD exhibits antibacterial properties, expanding its utility in various biological research applications. -
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. -
Cyanotoxin
Cylindrospermopsin, a cyanotoxin, is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA. Cylindrospermopsin induces hepatocellular hypertrophy, renal cellular hypertrophy, intracellular reactive oxygen species (ROS), DNA strand breaks, mitochondrial hyperpolarisation, ultrastructural damage, and altered gene expression in liver, kidney, and intestinal cells. Cylindrospermopsin can be used in research including hepatocellular carcinoma and water quality testing. -
Fluorochrome
Propidium Iodide (PI) is a nuclear staining agent that stains DNA. Propidium Iodide is an analogue of ethidine bromide that emits red fluorescence upon embedding in double-stranded DNA. Propidium Iodide cannot pass through living cell membranes, but it can pass through damaged cell membranes to stain the nucleus. Propidium Iodide has a fluorescence wavelength of 493/617 nm and a wavelength of 536/635 nm after Mosaic with DNA. Propidium Iodide is commonly used in the detection of apoptosis (apoptosis) or necrosis (necrosis), and is often used in flow cytometry analysis. -
Antibiotic
Erythromycin is a macrolide antibiotic that targets bacterial 50S ribosomal subunits, effectively inhibiting RNA-dependent protein synthesis by obstructing transpeptidation and translocation reactions. This compound demonstrates a broad spectrum of antimicrobial activity against various bacteria, making it valuable in microbiological research. Additionally, erythromycin has been shown to possess antitumor and neuroprotective properties, contributing to its usefulness in diverse areas of biomedical research. -
Skin Depigmenting Agent
Monobenzone is a potent skin depigmenting agent that primarily targets the enzyme ribonucleotide reductase (RNR) by inhibiting its regulatory subunit, RRM2. It effectively induces depigmentation, making it a valuable compound in vitiligo research. Additionally, Monobenzone demonstrates significant anti-leukemic properties, inhibiting the proliferation and DNA synthesis of acute myeloid leukemia (AML) cells, and promoting cell cycle arrest and apoptosis. These dual functionalities position Monobenzone as a critical reagent in both dermatological and oncology studies. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine hemisulfate is an acridine compound that functions primarily as a broad-spectrum antimicrobial agent and a Kir3.2 potassium channel blocker. Its mechanism involves insertion into bacterial DNA, thereby disrupting replication and transcription, which ultimately leads to bacterial lysis. Additionally, this compound is utilized in research to investigate the neurological phenotype associated with Down syndrome. Due to its ability to penetrate the stratum corneum and accumulate in the cell nucleus, prolonged exposure warrants caution due to potential oncogenic effects. -
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. -
DNA/RNA Synthesis Chemical
2-O-Methylcytosine is an O-alkylated analogue of cytosine, functioning as a DNA and RNA synthesis chemical. This modified nucleobase plays a critical role in the study of DNA alterations and epigenetic modifications. It is widely utilized in molecular biology research, particularly in the synthesis of modified nucleic acids and the investigation of nucleobase interactions. -
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.
