DNA Damage

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  1. Dxd

    DNA topoisomerase I inhibitor

    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  2. PARP1/PARP2 inhibitor

    E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ?50 and ?50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
  3. Hydroxy aryl aldehydes (HAA) inhibitor

    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  4. HDAC inhibitor

    Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM.
  5. FAS inhibitor

    FAS-IN-1 is a potent inhibitor of Fatty acid synthase (FAS) wtih IC50 of 10 nM, extracted from Patnet WO2012/064642Al.
  6. nudix hydrolase family inhibitor

    TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
  7. BLM helicase inhibitor

    ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLMfull-length and BLM636-1298, respectively.
  8. HCV NS5B polymerase inhibitor

    NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM.
  9. HDAC inhibitor

    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
  10. IRE1α inhibitor

    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  11. HCV NS5B polymerase inhibitor

    PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase.
  12. eukaryotic DNA polymerase α inhibitor

    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM.
  13. RSV polymerase inhibitor

    Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.
  14. prodrug of the topoisomerase inhibitor Daunorubicin

    Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
  15. Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
  16. Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
  17. PARP1 inhibitor

    Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
  18. Topoisomerase inhibitor

    Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.
  19. topoisomerase II inhibitor

    Daunorubicin (Daunomycin; RP 13057; Rubidomycin) is a topoisomerase II inhibitor with potent antineoplastic activities.
  20. GARFT inhibitor

    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
  21. Silvestrol aglycone enantiomer is a cyclopenta benzofuran core phenol.
  22. DNA topoisomerase I/II inhibitor

    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
  23. DNA synthesis inhibitor

    MB-7133 is a DNA synthesis inhibitor.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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