Catalog No.
Product Name
Application
Product Information
Citations
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DNA-PK Inhibitor
DNA-PK-IN-5 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting the catalytic subunit DNA-PKcs. This compound effectively disrupts tumor DNA repair mechanisms, promoting apoptosis in cancer cells. DNA-PK-IN-5 has been shown to enhance the sensitivity of tumor tissues to radiotherapy and addresses challenges related to agent resistance, providing a robust inhibitory effect on various solid tumors and hematological malignancies. -
DNA-PK Inhibitor
SU-11752 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), exhibiting an IC50 value of 0.13 μM. This compound also inhibits the PI3K p110γ kinase with an IC50 of 1.1 μM. By competitively binding to the ATP-site of DNA-PK, SU-11752 effectively disrupts intracellular DNA double-strand break repair mechanisms, thereby enhancing the sensitivity of cells to radiotherapy. This makes it a valuable tool in cancer research and therapy applications. -
DNA-PK Inhibitor
DNA-PK-IN-3 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), an essential component of DNA repair mechanisms. This compound enhances the efficacy of radiotherapy and chemotherapy while effectively inhibiting tumor growth. Additionally, DNA-PK-IN-3 has been shown to minimize damage to normal cells, thereby reducing associated side effects. Its potential applications extend to cancer research, providing valuable insights into therapeutic strategies targeting DNA repair pathways. -
DNA-PK Inhibitor
DNA-PK-IN-1 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), a key enzyme complex comprised of the Ku70/Ku80 heterodimer and the DNA-PK catalytic subunit (DNA-PKcs). This compound exhibits significant activity in inhibiting DNA-PK, making it a valuable tool for investigating DNA damage response and repair mechanisms in cancer research. Its application is particularly relevant in studies aimed at understanding tumor biology and developing targeted cancer therapies. -
DNA-PK Inhibitor
ZL-2201 free base is a highly selective inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 of 1 nM. This compound has significant implications in research applications focused on DNA repair mechanisms, cancer therapy, and radiation sensitization. ZL-2201 is ideal for studies investigating the modulation of DNA damage response pathways. -
DNA-PK inhibitor
DNA-PK-IN-14 is a potent selective inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 7.95 nM. This compound exhibits oral bioactivity and demonstrates potential as a radiosensitizer in cancer treatment. It can be utilized in research applications focusing on DNA repair mechanisms and the enhancement of radiotherapy efficacy. -
DNA-PK Inhibitor
DNA-PK-IN-4 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting DNA-PKcs activity. As an imidazolinone derivative, it effectively diminishes DNA repair capabilities in tumor cells, leading to increased apoptosis. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting DNA repair pathways. -
DNA-PK Inhibitor
DNA-PK-IN-10 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), a critical enzyme involved in the DNA damage response and repair mechanisms. This compound has demonstrated significant potential in the investigation of tumorigenesis, particularly in breast cancer and non-small cell lung cancer models. Its application in research may aid in understanding the roles of DNA-PK in cancer cell survival and resistance to therapies, providing insights for the development of targeted treatments. -
DNA-PKcs Inhibitor
IC-87361 is a selective inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs), serving as a potent radiosensitizer. By inhibiting the catalytic activity of DNA-PKcs, IC-87361 effectively disrupts non-homologous end joining (NHEJ) pathways involved in the repair of DNA double-strand breaks. This compound is particularly valuable in research related to lung cancer and melanoma, providing insights into therapeutic strategies that target DNA repair mechanisms. -
DNA-PK Inhibitor
DNA-PK-IN-6 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting DNA-PKcs activity. By inhibiting this kinase, DNA-PK-IN-6 significantly reduces the DNA repair capacity of tumor cells, thereby promoting apoptosis. This compound enhances the sensitivity of various solid tumors and hematological malignancies to radiotherapy, addressing challenges related to treatment resistance. Its applications are crucial for research in cancer therapeutics and treatment strategies. -
DNA-PK Inhibitor
OK-1035 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), exhibiting an IC50 value of 100 μM. It interferes with DNA double strand break repair mechanisms, thus providing valuable insights into cellular responses to DNA damage. This compound has potential applications in cancer research, particularly in studies focused on enhancing the efficacy of radiotherapy and chemotherapeutics. -
DNA-PK Inhibitor
NU-7163 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 of 0.19 μM and a Ki of 24 nM. This compound enhances the cytotoxic effects of ionizing radiation in the HeLa human tumor cell line, making it a valuable tool for research in cancer biology and therapeutic development. NU-7163 may be particularly relevant in studies exploring DNA repair mechanisms and enhancing the effectiveness of radiotherapy. -
eIF2B Activator
2BAct is a selective activator of the eukaryotic initiation factor 2B (eIF2B) with an EC50 of 33 nM. This compound effectively prevents neurological defects associated with a chronic integrated stress response, making it a valuable tool for research in neurobiology and stress response mechanisms. Additionally, 2BAct demonstrates enhanced solubility and improved pharmacokinetic properties compared to the eIF2B activator ISRIB trans-isomer. -
eIF Inhibitor
GCN2-IN-6 is a selective inhibitor of GCN2, exhibiting potent activity with an IC50 of 1.8 nM in enzymatic assays and 9.3 nM in cellular contexts. Additionally, this compound acts as an eIF2α kinase PERK inhibitor, demonstrating an IC50 of 0.26 nM enzymatically and 230 nM in cellular assays. GCN2-IN-6 also features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it valuable for biochemical research applications. -
eIF4e Inhibitor
eIF4E-IN-2 is a potent inhibitor targeting eukaryotic initiation factor 4E (eIF4E), with an IC50 of 13 nM. This compound effectively inhibits the proliferation of MDA-MB-361 breast cancer cells, thereby demonstrating its potential in cancer research. eIF4E-IN-2 can be utilized for studies investigating the role of eIF4E in breast cancer progression and therapeutic interventions. -
EIF2α Activator
EIF2α Activator 2 is a potent activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. It demonstrates significant antiproliferative activity, with IC50 values of 4.79 μM against K562 cells and 10.52 μM against peripheral blood mononuclear cells (PBMCs). This compound is primarily used in research focused on understanding the regulatory mechanisms of protein synthesis and cell proliferation. -
eIF4A3 Inhibitor
eIF4A3-IN-8 is a selective ATP-competitive inhibitor targeting eukaryotic initiation factor 4A3 (eIF4A3). This compound functions as a valuable chemical probe for investigating the role of eIF4A3 in mRNA processing and the exon junction complex (EJC). Its ability to modulate eIF4A3 activity makes it a useful tool for research into gene expression regulation and related biological pathways. -
eIF4E/eIF4G Interaction Inhibitor
(Z)-4EGI-1 is an inhibitor of the interaction between eIF4E and eIF4G, targeting translation initiation. With an IC50 of 43.5 μM and a Kd value of 8.74 μM, (Z)-4EGI-1 demonstrates significant binding affinity for eIF4E. This compound exhibits anticancer activity, making it a valuable tool for research in cancer biology and studies focused on the regulation of protein synthesis. -
eIF4F Inhibitor
eIF4A3-IN-18 is an effective eIF4F inhibitor that disrupts the assembly of the eIF4F translation complex. It demonstrates potent biological activity with EC50 values of 0.8 nM for myc-LUC, 35 nM for tub-LUC, and inhibits growth in MBA-MB-231 cells. Additionally, eIF4A3-IN-18 exhibits significant cytotoxicity towards RMPI-8226 cells, with an LC50 of 0.06 nM. This compound is valuable for research into the mechanisms of human cancer pathogenesis. -
eIF4F Inhibitor
eIF4A3-IN-12 is an eIF4F inhibitor, specifically disrupting the assembly of the eIF4F translation complex. With EC50 values of 4 nM for myc-LUC, 70 nM for tub-LUC, and 5 nM for inhibiting the growth of MBA-MB-231 cells, this compound demonstrates potent biological activity. eIF4A3-IN-12 is valuable for investigating human cancer pathogenesis and understanding the role of translation regulation in tumorigenesis. -
eIF4A3-IN-2 Less Active Enantiomer
(R)-eIF4A3-IN-2 is the less active enantiomer of eIF4A3-IN-2, a selective noncompetitive inhibitor of eukaryotic initiation factor 4A-3 (eIF4A3). With an IC50 of 110 nM, eIF4A3-IN-2 demonstrates significant inhibition of eIF4A3, impacting mRNA splicing and translation processes. This compound is useful in research applications focused on cancer biology, novel therapeutic pathways, and the regulation of gene expression. -
eIF4F Inhibitor
eIF4A3-IN-16 is a potent eIF4F inhibitor that selectively disrupts the assembly of the eIF4F translation complex. It demonstrates significant biological activity, inhibiting MBA-MB-231 cell growth with an EC50 of 1 nM. Additionally, eIF4A3-IN-16 affects myc-LUC and tub-LUC with EC50 values of 1 nM and 30 nM, respectively. This compound is applicable in research focused on triple negative breast cancer (TNBC). -
EIF2b Activator
Fosigotifator THAM sodium is a potent activator of eukaryotic initiation factor 2B (EIF2B), enhancing its stability and function. This compound is capable of penetrating the blood-brain barrier and demonstrates efficacy in boosting EIF2B activity, particularly in scenarios involving pathogenic vanishing white matter (VWM) mutations. As an integrated stress response inhibitor, Fosigotifator THAM sodium serves as a valuable tool in research focused on amyotrophic lateral sclerosis and related neurodegenerative conditions. -
eIF4e Inhibitor
eIF4E-IN-3 is a highly effective inhibitor of eukaryotic initiation factor 4E (eIF4E), a critical component in the protein synthesis initiation pathway. This compound demonstrates significant potential in investigating eIF4E-dependent diseases, particularly in cancer research. By modulating eIF4E activity, eIF4E-IN-3 offers valuable insights into the molecular mechanisms underlying tumorigenesis and may aid in the development of targeted therapeutic strategies. -
eIF4F Inhibitor
eIF4A3-IN-15 is a targeted inhibitor of the eIF4F translation complex, effectively disrupting its assembly. This compound demonstrates potent activity with EC50 values of 11, 700, and 120 nM against myc-LUC and tub-LUC, as well as growth inhibition in MBA-MB-231 cancer cells. eIF4A3-IN-15 is suitable for research applications focused on understanding the mechanisms underlying human cancer pathogenesis. -
eIF4F Inhibitor
eIF4A3-IN-9 is a potent eIF4F inhibitor that disrupts the formation of the eIF4F translation complex. Demonstrating EC50 values of 29 nM for myc-LUC, 450 nM for tub-LUC, and an effective growth inhibition in MBA-MB-231 cells, this compound serves as a valuable tool in the study of cancer biology. Its targeted action makes it suitable for investigating human cancer pathogenesis and exploring therapeutic strategies against malignancies. -
eIF Inhibitor
eIF4A3-IN-4 is a selective inhibitor of the eIF4A protein, exhibiting an IC50 value of 8.6 μM. This compound is relevant for research applications targeting the regulation of translation initiation and the modulation of gene expression. It has potential utility in studying cancer biology and other disorders related to abnormal protein synthesis. -
eIF4F Inhibitor
eIF4A3-IN-10 is an inhibitor of the eIF4F translation complex. It exhibits significant biological activity, with EC50 values of 35 nM for myc-LUC and 100 nM for growth inhibition in MBA-MB-231 cancer cells. This compound serves as a valuable tool in researching the pathogenesis of human cancers, particularly in the context of disrupted translation regulation associated with tumorigenesis. -
eIF4F Inhibitor
eIF4A3-IN-17 is an eIF4F inhibitor that disrupts the assembly of the eIF4F translation complex. It has demonstrated potent biological activity with EC50 values of 0.9 nM for myc-LUC, 15 nM for tub-LUC, and 1.8 nM for inhibiting the growth of MBA-MB-231 cells. This compound can be utilized in research focused on understanding human cancer pathogenesis and the mechanisms underlying oncogenic translation regulation. -
eIF4F Inhibitor
eIF4A3-IN-13 is an inhibitor of the eIF4F translation complex, functioning through disruption of its assembly. This compound exhibits potent biological activity, with EC50 values of 0.6 nM for myc-LUC, 15 nM for tub-LUC, and 0.4 nM for growth inhibition in MBA-MB-231 breast cancer cells. eIF4A3-IN-13 is a valuable tool for investigating the mechanisms of human cancer pathogenesis and exploring therapeutic strategies targeting translation regulation. -
eIF4F Inhibitor
eIF4A3-IN-11 is a potent inhibitor of the eIF4F translation complex. It effectively disrupts complex assembly, exhibiting EC50 values of 0.2 nM for myc-Luciferase, 4 nM for tubulin-Luciferase, and 0.3 nM for the inhibition of MBA-MB-231 cancer cell growth. This compound is valuable for investigating the molecular mechanisms underlying human cancer pathogenesis. -
eIF4A Inhibitor
eIF4A3-IN-14 is a selective inhibitor of eIF4A, a crucial component of the eIF4F translation complex. This compound demonstrates potent inhibitory activity with an EC50 of approximately 40 nM against myc-LUC and over 2000 nM against tub-LUC. eIF4A3-IN-14 is valuable for investigating tumorigenesis and the molecular mechanisms of translational regulation in cancer research. -
eIF Inhibitor
CMLD012612 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), designed to disrupt the translation initiation process in eukaryotic cells. This amidino-rocaglate compound features a hydroxamate group, demonstrating significant cytotoxicity in NIH/3T3 cells, with an IC50 value of 2 nM. By modifying the activity of the RNA helicase eIF4A, CMLD012612 exhibits promising anti-neoplastic properties, making it a valuable tool for cancer research and studies focused on translation regulation. -
EIF2b Activator
Fosigotifator is an orally active activator of eukaryotic initiation factor 2B (eIF2B), known for its ability to penetrate the blood-brain barrier. By stabilizing the eIF2B complex, Fosigotifator enhances its activity, particularly in the context of pathogenic vanishing white matter (VWM) mutations. As an integrated stress response inhibitor (ISRI), this compound is valuable for research in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS). -
eIF Inhibitor
CMLD012073 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), functioning through the mechanism of amidino-rocaglates. This compound effectively inhibits cell growth in NIH/3T3 cells with an IC50 value of 10 nM. CMLD012073 disrupts eukaryotic translation initiation by altering the activity of the RNA helicase eIF4A, making it a valuable tool for research applications related to protein synthesis and gene regulation. -
eIF Inhibitor
CMLD012072 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4A1 and eIF4A2 through RNA clamping. This amidino-rocaglate compound exhibits significant anti-neoplastic activity, making it a valuable tool for researching the role of eIF4A in cancer biology and therapeutic interventions. Its mechanism of action provides insight into the regulation of protein synthesis in neoplastic cells, facilitating further studies in oncology and molecular biology. -
eIF4A3 Inhibitor
eIF4A3-IN-7 is a potent inhibitor of the eIF4A3 protein, a key regulator of mRNA translation and splicing. This compound demonstrates significant potential for research in cancer and other dysproliferative diseases by modulating gene expression pathways. Its targeted mechanism of action may provide valuable insights into the role of eIF4A3 in tumorigenesis and other pathological conditions. -
eIF2α Activator
1,3-Bis[3,5-bis(trifluoromethyl)phenyl]urea is a potent activator of the eIF2α kinase heme-regulated inhibitor. It effectively reduces the levels of the eIF2·GTP·tRNAiMet ternary complex, thereby modulating protein synthesis. This compound also demonstrates significant inhibitory effects on cancer cell proliferation, making it a valuable tool in cancer research and investigations into cellular stress responses. -
SIRT2 Inhibitor
RK-9123016 is a selective inhibitor of SIRT2, effectively inhibiting its enzymatic activity with an IC50 of 0.18 µM, while showing no significant effect on SIRT1 or SIRT3 at concentrations up to 100 µM. This compound enhances the acetylation of eukaryotic translation initiation factor 5A (eIF5A), a known substrate of SIRT2, and is shown to decrease cell viability in human breast cancer cells, correlating with reduced expression of c-Myc. RK-9123016 is valuable for research into cancer biology and the role of sirtuins in cellular processes. -
SIRT1 Activator
Altissimacoumarin F is a terpenylated coumarin that acts as an activator of SIRT1, a protein implicated in cellular stress response and longevity. This compound, isolated from the stem bark of Ailanthus altissima, enhances SIRT1 activity while simultaneously decreasing p53 transcriptional activity. Altissimacoumarin F is valuable for research into age-related disorders and related pathways, providing insights into potential therapeutic strategies. -
SIRT1 Inhibitor
SIRT1-IN-6 is a selective SIRT1 inhibitor with an IC50 value of 9.7 μM. This compound effectively increases p53 acetylation, which is significant in regulating cell cycle and apoptosis. SIRT1-IN-6 is ideal for research applications related to neurodegenerative diseases and cancer, offering insights into potential therapeutic strategies for these conditions. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 16 (compound CT3) is an irreversible inhibitor that selectively targets trypanosomal topoisomerase II by stabilizing double-stranded DNA-enzyme cleavage complexes. This compound demonstrates significant brain penetration and exhibits oral bioavailability, making it a valuable tool for research focused on Chagas disease and related trypanosomal infections. Its distinct mechanism of action underscores its potential utility in exploring therapeutic strategies against these diseases. -
DNA Synthesis Inhibitor
Quinoprazine is a potent inhibitor of DNA synthesis, specifically targeting Vaccinia virus with an IC50 value of 10 μM. This compound demonstrates significant antimalarial activity against Plasmodium berghei and exhibits antiprion efficacy, effectively reducing levels of the pathogenic protein PrPSc. Quinoprazine's diverse biological activities make it a valuable tool for research in virology, parasitology, and prion disease studies. -
Topoisomerase II Inhibitor
Anti-Trypanosoma cruzi agent-9 is a potent inhibitor of topoisomerase II, effectively disrupting DNA replication and cellular division in target organisms. This compound exhibits significant biological activity against Trypanosoma cruzi, the causative agent of Chagas disease, as well as Leishmania donovani, which is responsible for leishmaniasis. It is a valuable tool for research applications aimed at understanding the mechanisms of these parasitic infections and developing novel therapeutic strategies. -
RSV Polymerase inhibitor
RSV L-protein-IN-3 is an inhibitor of respiratory syncytial virus (RSV) polymerase, displaying an IC50 value of 10.4 μM and an EC50 value of 2.1 μM against RSV. It demonstrates reduced cytotoxicity compared to the clinical agent Ribavirin, making it a suitable candidate for further research into treating RSV infections. This compound is valuable for studies focusing on antiviral mechanisms and drug development targeting RSV. -
RSV Polymerase Inhibitor
RSV L-protein-IN-4 is a noncompetitive inhibitor of the respiratory syncytial virus (RSV) polymerase, exhibiting an IC50 value of 0.88 μM. This compound demonstrates significant antiviral activity against various RSV strains, with an EC50 of 0.25 μM. RSV L-protein-IN-4 is essential for research into antiviral therapies targeting RSV infections. -
RSV Polymerase Inhibitor
RSV L-protein-IN-2 is a noncompetitive inhibitor of the Respiratory Syncytial Virus (RSV) polymerase, exhibiting an IC50 value of 4.5 μM. This compound demonstrates significant antiviral activity against long strains of RSV, with an EC50 of 1.3 μM. It is applicable in research focused on developing therapeutic strategies against RSV infections and understanding viral replication mechanisms. -
RNA-dependent RNA Polymerase Inhibitor
BPR3P0128 is a non-nucleoside inhibitor of RNA-dependent RNA polymerase (RdRp), demonstrating potent antiviral activity against various SARS-CoV-2 variants. It exhibits EC50 values of 0.62 μM for SARS-CoV-2 and 0.14 μM for HCoV-229E, effectively inhibiting virus replication within the submicromolar range. Additionally, BPR3P0128 shows synergistic effects when used in combination with Remdesivir, making it a promising candidate for further antiviral research against coronaviruses. -
Nucleoside Analog
5-Hydroxymethyl-2'-deoxyuridine is a nucleoside analog that serves as an effective inhibitor of DNA replication in various human leukemia cell lines, exhibiting IC50 values ranging from 1.7 to 5.8 μM. This compound has been shown to extend the survival of mice with L1210 leukemia, demonstrating its potential in cancer treatment research. Its unique properties make it a valuable tool for investigating mechanisms of cell replication and the biology of leukemia. -
HSV Polymerases Inhibitor
PNU-183792 is a potent inhibitor of herpes simplex virus (HSV) polymerases, classified as a 4-oxo-dihydroquinoline. It demonstrates broad-spectrum antiviral activity, exhibiting IC50 values of 0.69 μM for human cytomegalovirus (HCM), 0.37 μM for varicella zoster virus, and 0.58 μM for HSV polymerases. Importantly, PNU-183792 operates selectively, showing no activity against human α, γ, or δ polymerases. Additionally, it exhibits inhibitory effects on simian varicella virus (SVV), murine cytomegalovirus (MCMV), and rat cytomegalovirus (RCMV), making it a valuable tool for antiviral research.
