DNA Damage

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  1. HDAC1/CDK7 Inhibitor

    HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics.
  2. HDAC Inhibitor

    WMJ-J-09 is a potent HDAC inhibitor with sub-nanomolar activity, exhibiting IC50 values of 7.5 nM against HDAC1 and 3.9 nM against HDAC6, along with notable activity towards HDAC2, HDAC3, and HDAC8. This compound effectively disrupts the cell cycle and promotes apoptosis in cancer cells through the LKB1-AMPK-p38MAPK-p63-survivin signaling pathway. By inhibiting HDAC enzyme activity, WMJ-J-09 leads to the acetylation of critical proteins, thus contributing to the regulation of cell death in cancer models, such as HCT116 and FaDu cells.
  3. HDAC Inhibitor

    TH-6 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.115 µM for HDAC1, 0.135 µM for HDAC2, 0.242 µM for HDAC3, 0.138 µM for HDAC6, and 2.120 µM for HDAC8. This compound effectively inhibits cell migration and invasion while promoting apoptosis and inducing cell cycle arrest in the G2/M phase. TH-6 exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies.
  4. Topoisomerase II Inhibitor

    Topoisomerase II inhibitor 11 is a potent inhibitor of topoisomerase II, exhibiting an IC50 of 2.89 μM. It demonstrates significant antiproliferative activity, achieving 92.46% inhibition in the renal cancer cell line A498 with an IC50 of 3.5 μM. This compound induces cell cycle arrest at the G2/M phase, ultimately leading to inhibited cell proliferation and pro-apoptotic effects, making it an important tool for cancer research.
  5. HDAC Inhibitor

    HDAC-IN-36 is a potent HDAC (histone deacetylase) inhibitor that targets HDAC6 with an IC50 of 11.68 nM. This compound demonstrates significant biological activity by promoting apoptosis, enhancing autophagy, and inhibiting cellular migration. HDAC-IN-36 is applicable in cancer research, particularly in studies focusing on anti-tumor and anti-metastatic mechanisms in breast cancer.
  6. HDAC Inhibitor

    Trichostatin C is an HDAC inhibitor that plays a crucial role in modulating gene expression by preventing the deacetylation of histones. This compound exhibits significant anticancer activity, inducing apoptosis and causing cell cycle arrest in the G2/M phase, making it particularly effective against lung cancer and urothelial bladder cancer. Additionally, Trichostatin C promotes differentiation in Friend leukemic cells and demonstrates antifungal properties, highlighting its potential in various research applications related to cancer biology and fungal infections.
  7. 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.
  8. Purine Nucleoside Analog

    2'-O-Methyl-5-iodouridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its mechanism of action involves the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable tool in cancer research. This compound can be utilized in studies aimed at understanding the biochemical pathways of cancer and the development of novel therapeutic strategies.
  9. JMJD3/HDAC1/HDAC6 Inhibitor

    JMJD3/HDAC-IN-1 is a dual inhibitor targeting both Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylases HDAC1 and HDAC6. With an IC50 value of 16 nM for HDAC1, this compound induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, promoting apoptosis through cleavage of caspase-7 and PARP. JMJD3/HDAC-IN-1 demonstrates significant anti-cancer activity by inhibiting cell cloning, migration, and invasion, making it valuable in cancer research and therapeutic studies.
  10. Topoisomerase Inhibitor

    Cholesteryl hemisuccinate is a topoisomerase inhibitor with notable hepatoprotective and anticancer properties. It effectively mitigates acetaminophen-induced hepatotoxicity by preventing hepatic apoptosis and necrosis. Additionally, cholesteryl hemisuccinate interferes with DNA replication and repair mechanisms by inhibiting DNA polymerase and DNA topoisomerase, ultimately leading to reduced tumor growth. This compound is suitable for applications in cancer research and liver protection studies.
  11. Topoisomerase II Inhibitor

    Etoposide phosphate is a selective inhibitor of topoisomerase II, instrumental in disrupting DNA re-ligation processes. As the phosphate ester proagent of etoposide, it exhibits potent anti-cancer activity by inducing cell cycle arrest, apoptosis, and autophagy in cancer cells. This compound is primarily employed in cancer research to explore mechanisms of action and potential therapeutic strategies in oncology.
  12. HDAC3/p-STAT3 Inhibitor

    1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment.
  13. SIRT7 Inhibitor

    SIRT7 Inhibitor 97491 is a selective inhibitor of the SIRT7 enzyme, exhibiting an IC50 of 325 nM and effectively reducing its deacetylase activity in a dose-dependent manner. This compound enhances tumor suppression by stabilizing the p53 protein through acetylation at lysine residues K373 and K382. Additionally, SIRT7 Inhibitor 97491 promotes apoptosis via the caspase signaling pathway, making it a valuable tool for cancer research and studies focused on elucidating the role of SIRT7 in tumor progression.
  14. eIF4A Inhibitor

    CR-1-31-B is a synthetic rocaglate that serves as a potent inhibitor of the eukaryotic translation initiation factor eIF4A. By disrupting the interaction between eIF4A and RNA, CR-1-31-B impedes the initiation phase of protein synthesis. This compound has been shown to affect the association of Plasmodium falciparum eIF4A with RNA and induce apoptosis in neuroblastoma and gallbladder cancer cells, making it a valuable tool for studying mechanisms of protein synthesis and cancer biology.
  15. Topoisomerase II Inhibitor

    ICRF-193 is a potent inhibitor of DNA Topoisomerase II, disrupting DNA synthesis and inducing apoptosis in cancer cells. This compound exhibits significant anti-cancer and anti-inflammatory activities, making it valuable for research in oncology and inflammation. Additionally, ICRF-193 demonstrates cardioprotective properties against anthracycline-induced toxicity in cardiomyocytes. It is particularly relevant for studies focusing on acute promyelocytic leukemia, as well as broader investigations into cancer, infection, inflammation, and cardiovascular conditions.
  16. Purine Nucleoside Analog

    6-Azuridine is a purine nucleoside analog that acts as an effective activator of autophagic flux. It induces apoptosis through AMPK and p53 pathways, demonstrating significant antitumor and antiviral properties. This compound is valuable for research applications in cancer therapy and antiviral studies.
  17. 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.
  18. SIRT6 Activator

    SIRT6 activator 12q is a potent and selective small molecule that acts as an activator of SIRT6, exhibiting an IC50 of 0.58 μM, while demonstrating much lower activity against other sirtuins such as SIRT1-3 and SIRT5. This compound has been shown to inhibit cell growth and migration, induce apoptosis, and cause cell cycle arrest at the G2 phase. With its potential anticancer properties, SIRT6 activator 12q is a valuable tool for research in cancer biology and therapeutic development targeting SIRT6 pathways.
  19. 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.
  20. 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.
  21. Purine Nucleoside Analog

    N6-(2-Hydroxyethyl)adenosine is a purine nucleoside analog that targets the NF-κB/Smad signaling pathway. This compound demonstrates significant biological activities, including anti-hyperglycemic, antioxidant, antitumor, and anti-inflammatory effects. Additionally, it exhibits insecticidal properties, making it relevant for various research applications in pharmacology and toxicology. N6-(2-Hydroxyethyl)adenosine is noted for its oral bioactivity.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. Nucleoside Analog

    CNDAC hydrochloride is a nucleoside analog that exerts its effects by inducing DNA damage and promoting apoptosis in target cells. As a metabolite of the orally active agent Sapacitabine, CNDAC hydrochloride is utilized in research focused on understanding mechanisms of cytotoxicity and exploring potential therapeutic applications in cancer treatment. This compound serves as a valuable tool for studying the impact of nucleoside analogs on cellular processes and DNA integrity.
  32. PROTAC HDAC8 Degrader

    SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation.
  33. 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.
  34. 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.
  35. Nampt/SIRT1/PRDX5 Activator

    Myricanol is a diarylheptanoid that acts as a Nampt activator, enhancing SIRT1 and PRDX5 activities. This compound exhibits notable anti-inflammatory properties and mitigates glucocorticoid-induced muscle atrophy while regulating inflammatory mediators. Additionally, it demonstrates growth inhibition and promotes apoptosis in human lung adenocarcinoma A549 cells. Myricanol is also implicated in neuroprotection via autophagy-mediated clearance of microtubule-associated protein tau and contributes to cardiovascular health by inhibiting key signaling pathways such as PDGFRβ and NF-κB. Its activation of mitochondrial transcription factor A (TFAM) further supports anti-renal fibrosis effects and improves insulin sensitivity through AMPK activation.
  36. 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.
  37. Topoisomerase Inhibitor

    Amonafide L-malate is a topoisomerase II inhibitor that functions as a DNA intercalator. This compound induces apoptotic signaling by disrupting the interaction between topoisomerase II and DNA, leading to inhibited DNA replication and cell proliferation. Amonafide L-malate is utilized in cancer research to study mechanisms of apoptosis and the effects of topoisomerase inhibition on tumor cells.
  38. HDAC Inhibitor

    HDAC-IN-37 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.0551 μM for HDAC1, 1.24 μM for HDAC3, 0.948 μM for HDAC8, and 34.2 μM for HDAC6. This compound effectively increases histone acetylation through a slow-off binding mechanism. Additionally, HDAC-IN-37 disrupts the transition from the G1 phase to the S phase of the cell cycle and promotes early apoptosis in various cell types, making it a valuable tool for research in cancer biology and therapeutic development.
  39. c-Met/HDAC Inhibitor

    c-Met/HDAC-IN-3 is a dual inhibitor targeting c-Met and histone deacetylase 1 (HDAC1), exhibiting IC50 values of 12.50 nM and 26.97 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. c-Met/HDAC-IN-3 serves as a valuable tool for research in cancer biology and therapeutic development, particularly in studies focused on synergistic inhibition of oncogenic pathways.
  40. PARP-1/2/TNKS1/2 Inhibitor

    PARP1/2/TNKS1/2-IN-1 is an inhibitor targeting PARP-1, PARP-2, TNKS1, and TNKS2, with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM, and 4.15 nM, respectively. This compound demonstrates significant antitumor activity and promotes apoptosis, making it a valuable tool for research focused on cancer biology and therapeutic strategies. Its dual inhibitory action can facilitate the exploration of cellular repair mechanisms and enhance the understanding of poly(ADP-ribose) polymerases in cancer treatment.
  41. HDAC6 Inhibitor

    HDAC6-IN-4 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 23 nM. This compound promotes apoptosis in cancer cells and demonstrates significant antitumor efficacy while exhibiting minimal toxicity. HDAC6-IN-4 is valuable for research in cancer biology, particularly in studies focused on epigenetic regulation and therapeutic development.
  42. HDAC Inhibitor

    HDAC-IN-31 is a selective and orally active histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 84.90 nM for HDAC1, 168.0 nM for HDAC2, 442.7 nM for HDAC3, and greater than 10,000 nM for HDAC8. This compound induces apoptosis and triggers G2/M phase cell cycle arrest, demonstrating significant antitumor efficacy. HDAC-IN-31 is applicable in research focused on diffuse large B-cell lymphoma and other cancer studies.
  43. Topoisomerase/HDAC Inhibitor

    Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation.
  44. Nucleoside Analogue

    LCB-2122 is a nucleoside analogue that mimics adenosine and features a C2'-stereogenic all-carbon quaternary center. This compound exhibits protective effects against Doxorubicin-induced apoptosis in cardiomyocytes with an IC50 of 0.5 μM and also mitigates apoptosis induced by Imatinib. LCB-2122 activates AMPK signaling pathways, promoting the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase (ACC), while reducing mitochondrial damage linked to Doxorubicin treatment. Its biological activities make LCB-2122 a valuable reagent for investigating mechanisms related to heart failure.
  45. mTOR/HDAC6 Inhibitor

    mTOR/HDAC6-IN-1 is a potent dual inhibitor targeting mTOR and HDAC6, exhibiting IC50 values of 133.7 nM and 56 nM, respectively. This compound is known to induce significant autophagy and apoptosis while suppressing cell migration. It holds potential for research applications in triple-negative breast cancer (TNBC) studies, offering insights into the interplay between these critical pathways in cancer progression.
  46. HDAC Inhibitor

    HDAC-IN-59 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in cancer research. This compound promotes the generation of reactive oxygen species (ROS), leading to DNA damage and the induction of apoptosis via the mitochondria-related pathway. Additionally, HDAC-IN-59 effectively disrupts the cell cycle at the G2/M phase, making it a valuable tool for studying the mechanisms of cell growth regulation and apoptosis in various cancer models.
  47. JAK/HDAC Inhibitor

    JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies.
  48. c-Met/HDAC Inhibitor

    c-Met/HDAC-IN-2 is a highly potent dual inhibitor targeting c-Met and histone deacetylases (HDACs), exhibiting IC50 values of 18.49 nM for HDAC1 and 5.40 nM for c-Met. This compound demonstrates significant antiproliferative effects against various cancer cell lines, notably inducing G2/M-phase cell cycle arrest and apoptosis in HCT-116 cells. c-Met/HDAC-IN-2 is a valuable tool for investigating mechanisms of anti-cancer resistance and exploring therapeutic strategies in oncology research.
  49. HDAC inhibitor

    HDAC-IN-67 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. Its significant antitumor activity makes HDAC-IN-67 a valuable tool for cancer research and a potential candidate for therapeutic development.
  50. PIM-1/HDAC Inhibitor

    PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis.

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