Catalog No.
Product Name
Application
Product Information
Citations
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PARP-1 Inhibitor
PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM, targeting the PARP-1 enzyme to modulate DNA damage response pathways. It exhibits significant anti-proliferative effects in both rat (C6) and human (U87MG) glioma cell lines by promoting PARP cleavage and inducing reactive oxygen species (ROS), ultimately leading to increased cell apoptosis. Additionally, PARP1-IN-46 effectively inhibits glioma cell migration, invasion, and colony formation, making it a valuable tool for research on glioma biology and potential therapeutic strategies. -
PROTAC HDAC6 Degrader
PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways. -
HDAC4 Inhibitor
HDAC4-IN-1 is a selective inhibitor of histone deacetylase 4 (HDAC4), demonstrating an IC50 of 0.077 μM. This compound has been shown to enhance caspase-mediated apoptosis, highlighting its potential in anticancer applications. HDAC4-IN-1 is a valuable tool for research into drug combinations aimed at increasing the efficacy of cancer therapies. -
IRE1 Inhibitor
3-Ethoxy-5,6-dibromosalicylaldehyde is a selective non-competitive inhibitor of IRE1, including IRE1α, with an IC50 of approximately 0.12 μM for human IRE1α-cyto. This compound effectively inhibits XBP-1 splicing and induces apoptosis in various cellular contexts. It has been shown to upregulate TXNIP mRNA expression while downregulating TXN expression levels. Additionally, 3-ethoxy-5,6-dibromosalicylaldehyde exhibits promising anticancer activity against pancreatic cancer and significantly inhibits the replication of chikungunya virus, making it a valuable tool for research in apoptosis and viral biology. -
HDAC6 Inhibitor
HDAC6-IN-45 is a selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 15.2 nM. This compound has been shown to promote neurotrophic effects by enhancing the expression of GAP43 and Beta-3 tubulin, while also activating the Nrf2 signaling pathway. Further research applications include its ability to mitigate H2O2-induced reactive oxygen species production, inhibit apoptosis in PC12 cells, and confer neuroprotective effects in SCOP-induced zebrafish models of Alzheimer's disease. Additionally, HDAC6-IN-45 exhibits antioxidant properties and possesses favorable blood-brain barrier permeability. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-2 is a potent dual inhibitor targeting topoisomerase II (Topo II) and histone deacetylases (HDAC). This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for investigating the mechanisms of tumorigenesis and potential therapeutic interventions. Research applications include studies on cancer biology, drug development, and the modulation of epigenetic regulators. -
FLT3/HDAC Inhibitor
FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies. -
HDAC Inhibitor
HDAC-IN-81 is a potent HDAC1 inhibitor, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-cancer activity by effectively inhibiting cell proliferation and inducing apoptosis in cancer cells. It serves as a valuable tool for research applications in cancer biology and epigenetic regulation. -
HDAC Inhibitor
Valproic acid magnesium is an orally active histone deacetylase (HDAC) inhibitor that exhibits an IC50 range of 0.5 to 2 mM, specifically inhibiting HDAC1 with an IC50 of 400 μM while promoting the proteasomal degradation of HDAC2. This compound activates Notch1 signaling and demonstrates anti-proliferative effects in small cell lung cancer (SCLC) cells. Valproic acid magnesium has diverse therapeutic applications, including the treatment of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and the prevention of migraine headaches. -
HDAC Inhibitor
Nanatinostat TFA is a potent, orally active inhibitor of class I histone deacetylases (HDACs), with IC50 values of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. It demonstrates reduced activity against HDAC5 and HDAC6, with IC50 values of 200 nM and 2100 nM, respectively. Nanatinostat TFA effectively induces apoptosis in myeloma cells and exhibits significant anticancer properties against various malignancies, including advanced solid tumors and colorectal cancer. Its selective inhibition of HDACs positions it as a valuable compound for cancer research and therapeutic development. -
PI3K/HDAC Inhibitor
Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways. -
DNA Topoisomerase II Inhibitor
DNA Topoisomerase II Inhibitor 1 is a potent inhibitor of DNA topoisomerase II, a crucial enzyme involved in DNA replication and maintenance. This compound exhibits significant anti-proliferative activity by inducing apoptosis and causing cell cycle arrest at the sub-G1 phase. It serves as a valuable tool for research in cancer biology and therapeutic studies targeting cell growth and survival pathways. -
PARP 2 Inhibitor
PARP-2-IN-2 is a potent inhibitor of PARP-2, exhibiting an IC50 value of 0.057 μM. This compound effectively induces cell cycle arrest and apoptosis in MCF-7 breast cancer cells, highlighting its potential as a therapeutic agent in cancer research. PARP-2-IN-2 is valuable for investigations into cancer biology and therapeutic strategies targeting DNA repair mechanisms. -
HDAC Inhibitor
MC2625 is a potent histone deacetylase (HDAC) inhibitor, specifically targeting HDAC3 and HDAC6 with IC50 values of 80 nM and 11 nM, respectively. This compound effectively increases levels of acetylated histone H3 and acetylated tubulin, promoting apoptosis in cancer stem cells (CSCs) and inhibiting their growth. MC2625 serves as a valuable tool for research focused on cancer therapeutics and the role of epigenetics in tumor biology. -
Sirtuin Inhibitor
Sirt1/2-IN-4 is a potent triple inhibitor of the sirtuin family, specifically targeting SIRT1 and SIRT2 with IC50 values of 1.2 μM and 1.9 μM, respectively, and showing moderate inhibition of SIRT3 at 18.6 μM. This compound effectively prevents the deacetylation of p53, highlighting its potential role in cancer research. Its ability to modulate sirtuin activity makes it a valuable tool for investigating the biological implications of sirtuin inhibition in various cancer models. -
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. -
Purine Nucleoside Analog
TLR7 Agonist 9 is a purine nucleoside analog that specifically activates Toll-like receptor 7 (TLR7). This compound demonstrates immunostimulatory properties, making it suitable for research in cancer and infectious disease. Additionally, TLR7 Agonist 9 features an alkyne group, facilitating its use in click chemistry for the copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
MTH1 Substrate
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is a reactive oxidized guanine nucleotide that serves as a substrate for MTH1 and other pyrophosphohydrolases. This compound is known to act as a mutagen, integrating into DNA and leading to A:T to C:G transversions, which can contribute to genomic instability. Additionally, 8-Oxo-dGTP can provoke oxidative DNA modifications, strand breaks, and the promotion of apoptosis, particularly in mth1-deficient organisms. Its accumulation is linked to various biological processes and is extensively utilized in research on carcinogenesis, neurodegenerative diseases, and other pathologies. -
SIRT1 Activator
SRT 1720 dihydrochloride is a selective activator of SIRT1, exhibiting an EC50 of 0.10 μM. This compound demonstrates lower activity toward SIRT2 and SIRT3, making it an important tool for investigating SIRT1-related biological pathways. Its ability to modulate SIRT1 activity is particularly relevant in studies of metabolism, aging, and neuroprotection. -
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. -
DNA/RNA Synthesis Chemical
5-Propargylamino-3'-azidomethyl-dUTP functions as a nucleoside analogue in DNA and RNA synthesis. This reagent is compatible with copper-catalyzed azide-alkyne cycloaddition (CuAAC) and strain-promoted alkyne-azide cycloaddition (SPAAC), making it suitable for bioconjugation applications. Researchers can utilize this compound in diverse applications, including DNA synthesis and sequencing, owing to its azide and alkyne functionalities that facilitate modular addition of biomolecules. -
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. -
DNA/RNA Synthesis
RNAP-σ interaction inhibitor-1 is a specific inhibitor of RNA polymerase-sigma factor interactions, playing a crucial role in DNA and RNA synthesis. This compound demonstrates significant antibacterial activity against Streptococci, with minimal inhibitory concentration (MIC) values ranging from 1 to 2 µg/mL. It is a valuable tool for research applications focused on bacterial transcription mechanisms and the development of novel antibacterial agents. -
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 Polymerase
Tth DNA polymerase is a thermostable DNA polymerase derived from Thermus thermophilus, primarily targeting DNA synthesis. It exhibits high fidelity and robust activity at elevated temperatures, making it ideal for applications such as PCR and DNA sequencing. This enzyme is essential for researchers requiring efficient amplification and accurate DNA replication in challenging experimental conditions. -
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.
