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Topoisomerase Inhibitor
Cholesterol hemisuccinate Tris salt is a topoisomerase inhibitor that exhibits hepatoprotective and anticancer properties. This compound effectively mitigates acetaminophen-induced hepatotoxicity and prevents subsequent hepatic apoptosis and necrosis. By inhibiting DNA polymerase and DNA topoisomerase, it disrupts DNA replication and repair processes, ultimately inhibiting cell division and tumor growth. Additionally, this compound is suitable for buffer preparation in various laboratory applications. -
Telomerase Inhibitor
Imetelstat is a 13-mer oligonucleotide that functions as a competitive inhibitor of telomerase. By binding with high affinity to the RNA template region of human telomerase, Imetelstat induces apoptosis in cancer cells. This compound selectively eliminates hematopoietic stem cells in myelofibrosis, impairing the ability of cancer cells to maintain telomere length and ultimately inhibiting cell proliferation. Imetelstat's unique mechanism makes it a valuable tool for research applications focused on telomerase activity and cancer therapeutics. -
DNA-PK/p110α Inhibitor
PIK-75 is a selective inhibitor of DNA-PK and p110α, exhibiting IC50 values of 2 nM and 5.8 nM, respectively, while demonstrating over 200-fold greater potency against p110α compared to p110β (IC50 = 1.3 μM). This compound effectively induces apoptosis, making it a valuable tool for research in cancer biology and therapies targeting DNA repair pathways. Its specificity for these kinases facilitates investigations into their roles in cellular processes and potential therapeutic interventions. -
ATR Inhibitor
AD1058 is a selective, orally active inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR) with an IC50 of 1.6 nM. This compound demonstrates significant anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis in various cancer models. AD1058 is particularly relevant for research focused on advanced malignancies and brain metastases, providing a valuable tool for investigating therapeutic strategies in these challenging areas. -
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. -
eIF4A Inhibitor
Didesmethylrocaglamide is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a key player in the regulation of protein synthesis. This compound demonstrates significant growth-inhibitory activity with an IC50 of 5 nM, effectively suppressing various growth-promoting signaling pathways and inducing apoptosis in tumor cells. Didesmethylrocaglamide is primarily utilized in cancer research to explore its potential therapeutic applications in oncology. -
eIF4A Inhibitor
Rohinitib is a selective inhibitor of eIF4A, a critical protein involved in the regulation of translation initiation. It has demonstrated the ability to induce apoptosis in acute myeloid leukemia (AML) cell lines and effectively reduces leukemia burden in AML xenograft models. Rohinitib is a valuable tool for investigating the mechanisms of AML and exploring potential therapeutic strategies. -
Topoisomerase Inhibitor
Alternariol is a mycotoxin that functions as an inhibitor of topoisomerase I and II. This compound exhibits biological activities such as inducing apoptosis, triggering cell cycle arrest, and suppressing innate immune responses, making it valuable for cancer research. Additionally, Alternariol has shown weak estrogenic and antiandrogen effects, along with genotoxic and mutagenic properties, which are relevant to studies on endocrine disruption and its implications in toxicology. -
HDAC Inhibitor
DL-Sulforaphane N-acetyl-L-cysteine is an orally active inhibitor of histone deacetylases (HDACs) and a stable metabolite of sulforaphane. This compound enhances autophagy-mediated reduction of α-tubulin expression via the ERK signaling pathway, making it a valuable tool in cancer research. Its improved blood-brain barrier permeability and extended half-life support its potential in neurobiological studies and therapeutic applications. -
PARP Inhibitor
Niraparib tosylate hydrate is a potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 3.8 nM and 2.1 nM, respectively. This compound functions by disrupting the DNA repair mechanism, leading to the accumulation of DNA damage and subsequent activation of apoptosis. Niraparib tosylate hydrate demonstrates significant anti-tumor activity, making it a valuable tool for cancer research, particularly in studies focused on DNA repair pathways and therapeutic resistance. -
HDAC Inhibitor
Panobinostat lactate is a potent, orally active non-selective histone deacetylase (HDAC) inhibitor. It exhibits significant antineoplastic activity and has been shown to disrupt HIV latency effectively. Additionally, Panobinostat lactate induces apoptosis and autophagy in various cell types. This reagent is valuable for studying refractory or relapsed multiple myeloma and exploring HDAC inhibition in cancer research. -
DNA Topoisomerase I Inhibitor
Podocarpusflavone A is a selective inhibitor of DNA topoisomerase I, demonstrating notable anti-proliferative effects. It has been shown to induce apoptosis in MCF-7 breast cancer cells, suggesting its potential as an anti-tumor agent. This compound is suitable for research applications focused on cancer biology and the mechanistic exploration of cell growth regulation. -
HDAC Inhibitor
Purinostat mesylate is a selective inhibitor of histone deacetylases (HDACs), effectively targeting class I and class IIb HDACs with IC50 values ranging from 0.81 to 11.5 nM. This compound induces apoptosis and influences the cell cycle in LAMA84 and 188 BL-2 cell lines, demonstrating potent anti-leukemic effects in vivo. Purinostat mesylate serves as a valuable tool for researching lymphoblastic leukemia and its therapeutic potential. -
PARP1/2 Inhibitor
Mefuparib hydrochloride is a selective inhibitor of PARP1 and PARP2, demonstrating substrate-competitive activity with IC50 values of 3.2 nM and 1.9 nM, respectively. This potent compound induces apoptosis and exhibits significant anticancer effects in both in vitro and in vivo models. It is valuable for research in cancer therapeutics and cellular response mechanisms to DNA damage. -
SIRT6/SIRT2 Inhibitor
SIRT2/6-IN-1 is a dual inhibitor of SIRT6 and SIRT2 with IC50 values of 106 μM and 114 μM, respectively. This compound enhances histone H3K9 acetylation, promotes glucose uptake, and decreases TNF-α secretion in cellular models. SIRT2/6-IN-1 provides valuable insights for research into metabolic regulation and inflammatory responses, making it a useful tool for studying the roles of sirtuins in cellular processes. -
Topoisomerase I/II Inhibitor
SelB-1 is a dual inhibitor targeting Topoisomerase I and II, demonstrating significant anticancer activity. This compound is particularly useful in the study of prostate and colon cancers. Additionally, SelB-1 induces autophagy gene expression and lipid peroxidation, while effectively lowering glutathione (GSH) levels, providing insights into its mechanistic roles in cancer biology. -
PARP1 Inhibitor
Palacaparib is a potent inhibitor of PARP1, demonstrating over 8000-fold selectivity for PARP1 relative to PARP2, PARP3, PARP5a, and PARP6. It functions by selectively inhibiting PARP1 and trapping it at sites of single-strand breaks (SSBs), impeding DNA repair. This compound is investigated primarily for its anti-cancer properties, particularly in research related to HRD+ breast cancer and various advanced solid tumors. -
MTH1 Inhibitor
TH287 hydrochloride is a highly potent and selective inhibitor of MTH1, exhibiting an IC50 of 0.8 nM. It demonstrates significant selectivity for MTH1 over related enzymes, showing no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase, and ITPA at concentrations of 100 µM. This compound is valuable for cancer research, particularly in the exploration of novel chemotherapeutic strategies targeting MTH1's role in tumor metabolism. -
RNA Polymerase Inhibitor
MRL-436 is an RNA polymerase inhibitor that exhibits significant antibacterial activity against Rifampicin-resistant strains. Its mechanism of action involves targeting residue 622 of the RNA polymerase β' subunit and the RNAP ω subunit. This compound is particularly valuable for research involving antibiotic resistance and the study of bacterial transcription mechanisms. -
SIRT1/3 Inhibitor
SPC-180002 is a dual inhibitor of SIRT1 and SIRT3, exhibiting IC50 values of 1.13 μM and 5.41 μM, respectively. This compound disrupts redox homeostasis through reactive oxygen species (ROS) generation, resulting in enhanced stability of the p21 protein and consequential mitochondrial dysfunction. SPC-180002 effectively inhibits cell cycle progression and reduces cancer cell proliferation, while also activating the Nrf2 signaling pathway, making it a valuable tool for cancer research and studies on metabolic dysregulation. -
SIRT2/Hsp70 Inhibitor
YM-08 is a selective inhibitor of SIRT2 and Hsp70, exhibiting an IC50 of 19.9 μM for SIRT2. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases and cellular stress responses. Its dual inhibitory activity allows for investigation into SIRT2 and Hsp70's roles in various biological processes and potential therapeutic applications. -
HSP70/SIRT2 Inhibitor
HSP70/SIRT2-IN-2 is a dual inhibitor targeting SIRT2 and HSP70, demonstrating an IC50 of 45.1±5.0 μM for SIRT2. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to simultaneously inhibit these two proteins positions HSP70/SIRT2-IN-2 as a useful candidate for studies focused on tumor progression and potential therapeutic strategies. -
HDAC1/HDAC2 Inhibitor
MRLB-223 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent activity against tumor cells. It induces histone hyperacetylation and activates the intrinsic apoptotic pathway, leading to tumor cell apoptosis and degradation of Bcr-Abl in a caspase-dependent manner. Notably, MRLB-223 mediates p53-independent cell death in Bcr-Abl-expressing myeloid cells and shows efficacy in animal models of Eμ-myc lymphoma. This compound is valuable for research focusing on the mechanisms of lymphomagenesis and therapeutic strategies for Eμ-myc lymphoma. -
ATR Inhibitor
ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer. -
RNA-dependent RNA-polymerases Inhibitor
GS-443902 trisodium is a potent inhibitor of RNA-dependent RNA polymerases (RdRp), specifically targeting respiratory syncytial virus (RSV) and hepatitis C virus (HCV) RdRp with IC50 values of 1.1 μM and 5 μM, respectively. As the active triphosphate metabolite of Remdesivir (GS-5734), this compound is essential for research focused on viral replication mechanisms and the development of antiviral therapies. Its ability to effectively inhibit RdRp activity makes it a valuable tool for studies in virology and drug discovery. -
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. -
RNA Polymerase II/III Inhibitor
β-Amanitin is a cyclic peptide toxin that specifically targets and inhibits RNA Polymerase II and III, crucial enzymes in eukaryotic transcription. By obstructing these polymerases, β-Amanitin effectively halts protein synthesis, making it a valuable reagent in research focused on gene expression and transcription regulation. Additionally, its ability to induce cytotoxicity positions β-Amanitin as a potential component in antibody-drug conjugates (ADCs) for targeted therapeutic applications. -
RSV Polymerase Inhibitor
JNJ-8003 is a highly potent, orally active non-nucleoside inhibitor of respiratory syncytial virus (RSV) polymerase, exhibiting an IC50 of 0.29 nM. It specifically targets the L protein of the polymerase complex, effectively blocking the transcription and replication of the viral genome by inhibiting RNA-dependent RNA polymerase (RdRp) activity, with an IC50 of 0.67 nM. In vitro studies demonstrate subnanomolar efficacy, and it has shown significant effectiveness in mouse and neonatal lamb models. JNJ-8003 is a valuable reagent for investigating RSV biology and developing antiviral therapies. -
Topoisomerase Inhibitor
Hycanthone is a potent topoisomerase inhibitor that functions as a thioxanthenone DNA intercalator. It effectively inhibits RNA synthesis and the activity of DNA topoisomerases I and II, leading to a reduction in nucleic acid biosynthesis. Additionally, Hycanthone demonstrates significant inhibition of apurinic endonuclease-1 (APE1) through direct protein binding, with a binding affinity (KD) of 10 nM. This compound is recognized as a bioactive metabolite of Lucanthone and is noted for its anti-schistosomal properties, making it valuable in related research applications. -
DNA Polymerase β Inhibitor
Prunasin is a specific inhibitor of DNA Polymerase β, showing an IC50 value of 98 μM in rat models. As an orally active cyanogenic glucoside and a principal metabolite of Amygdalin, Prunasin exhibits notable anti-inflammatory and anti-fibrotic properties. This compound is valuable for research into conditions such as liver fibrosis, facilitating investigations into therapeutic strategies targeting DNA repair and fibrotic processes. -
Topoisomerase Inhibitor
Netropsin dihydrochloride is a potent topoisomerase inhibitor that functions as a minor-groove binder. It effectively inhibits the catalytic activity of isolated topoisomerases, disrupting the stabilization of cleavable complexes associated with topoisomerase I and II in the nucleus. Additionally, netropsin dihydrochloride exhibits notable antibacterial and antiviral properties, making it valuable for various research applications, including studies on DNA topology and therapeutic interventions against microbial infections. -
Telomerase Inhibitor
Braco-19 trihydrochloride is a potent telomerase inhibitor that disrupts telomerase capping and catalytic activity. By acting as a G-quadruplex binding ligand, Braco-19 stabilizes G-quadruplex formation at the 3' telomeric DNA overhang, leading to rapid cellular senescence or selective cell death. Additionally, Braco-19 demonstrates efficacy as an inhibitor of HAdV virus replication, making it a valuable tool for research in cancer biology and virology. -
Polθ/PARP Inhibitor
Polθ/PARP-IN-1 is a potent dual inhibitor targeting DNA polymerase theta (Polθ) and poly (ADP-ribose) polymerase (PARP), exhibiting IC50 values of 45.6 nM and 5.4 nM, respectively. This compound demonstrates significant antiproliferative activity by inducing apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage. Polθ/PARP-IN-1 is applicable in cancer research and may contribute to therapeutic strategies targeting tumorigenesis. -
DNA Polymerase Inhibitor
3,4-Dihydroxybenzylamine hydrobromide is a DNA polymerase inhibitor that exhibits cytotoxic effects in melanoma cells. This compound demonstrates significant growth inhibitory activity across various melanoma cell lines, with efficacy correlated to the levels of tyrosinase activity. Its unique mechanism makes it a valuable tool for investigating cellular processes related to DNA replication and repair in cancer research. -
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. -
MTH1 Inhibitor
BAY-707 is a potent and selective inhibitor of MTH1 (NUDT1) that functions through a substrate-competitive mechanism with an IC50 of 2.3 nM. This compound exhibits a favorable pharmacokinetic profile compared to other MTH1 inhibitors and demonstrates good tolerability in mouse models. Although BAY-707 has shown effective inhibition of MTH1, it does not exhibit significant anticancer activity in either in vitro or in vivo studies, making it suitable for research into MTH1 function and related pathways. -
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. -
Topoisomerase II Inhibitor
F-14512 is a topoisomerase II inhibitor that selectively targets cancer cells via the polyamine transport system. By enhancing the interaction of polyamines with DNA, F-14512 effectively inhibits topoisomerase II, leading to significant DNA damage and subsequent cellular cytotoxicity, particularly in cells exhibiting high PTS activity. This compound has demonstrated potent antitumor efficacy in the MX1 breast tumor xenograft model, making it a valuable tool for researching breast cancer and exploring mechanisms of drug resistance in oncological studies. -
Viral DNA Polymerase Inhibitor
Foscarnet trisodium hexahydrate is a viral DNA polymerase inhibitor that reversibly suppresses viral replication. It is primarily utilized as an antiherpesvirus agent, demonstrating efficacy in the treatment of cytomegalovirus retinitis. This compound is valuable for researchers studying viral infections and developing antiviral therapies. -
Poly(A) polymerase Inhibitor
2'-Deoxyadenosine 5'-diphosphate disodium (dADP disodium) acts as an inhibitor of bacterial poly(A) polymerase. This compound is particularly useful in the synthesis of deoxyadenosine oligonucleotides when utilized with Escherichia coli polynucleotide phosphorylase and other related enzymes. Its role in inhibiting poly(A) polymerase makes it valuable for studies in RNA metabolism and gene regulation research. -
DNA Polymerase Inhibitor
ddATP trisodium solution (100 mM) serves as a chain-elongating inhibitor of DNA polymerase. As an active metabolite of 2',3'-dideoxyinosine, it is primarily utilized in the Sanger method for DNA sequencing. Additionally, this reagent is valuable for studying viral infections and other applications in molecular biology research. -
DENV Polymerase Inhibitor
NITD-2 is a selective inhibitor of dengue virus (DENV) polymerase, specifically targeting the RNA-dependent RNA polymerase (RdRp) to impede RNA elongation. This compound exhibits potent antiviral activity against DENV, making it a valuable tool for research focused on understanding dengue virus replication and developing therapeutic strategies. Its limited ability to penetrate cell membranes can be an important consideration for in vitro experimental design. -
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 Polymerase α Inhibitor
NSC639828 is a potent inhibitor of DNA polymerase α, exhibiting an IC50 of 70 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. NSC639828 can be utilized to investigate the role of DNA polymerase α in tumorigenesis and to explore potential therapeutic strategies in cancer treatment. -
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 Polymerase Inhibitor
Acyclovir triphosphate sodium is a potent inhibitor of viral DNA polymerase, functioning as a competitive analogue of deoxyguanosine triphosphate (dGTP). This compound also exhibits inhibitory activity against HIV-1 reverse transcriptase, leading to the termination of viral DNA synthesis. Acyclovir triphosphate sodium is valuable for research applications in virology and the study of antiviral mechanisms.

