DNA Damage

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  1. Teniposide is a semisynthetic derivative of podophyllotoxin with antineoplastic activity.
  2. HIV reverse transcriptase inhibitor

    Tenofovir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV in the blood.
  3. Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity.
  4. DNA topoisomerase I inhibitor

    Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor.
  5. Trifluridine is an anti-herpesvirus antiviral drug, used primarily on the eye. It was sold under the trade name, Viroptic, by Glaxo Wellcome, now merged into GlaxoSmithKline.
  6. HDAC6 inhibitor

    Tubacin (tubulin acetylation inducer) is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM.
  7. nucleoside analogue reverse transcriptase inhibitor

    Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.
  8. ATM inhibitor

    CP-466722 is a specific ATM inhibitor that inhibits cellular ATM-dependent phosphorylation events and disruption of ATM function resulted in characteristic cell cycle checkpoint defects.
  9. β-1,3-Glucan Synthase Inhibitor

    Pneumocandin B0 is the major analogue of a family of lipopeptides isolated from several species of several different genera, notably Cryptosporiopsis, Glarea and Pezicula. Pneumocandin B0 is a potent antifungal and acts by inhibition of the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
  10. Transcriptase inhibitor

    Abacavir is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
  11. Guanosine 5′-triphosphate (GTP), a purine trinucleotide, is a substrate for RNA polymerases and a wide range of GTPase including G-protein coupled receptor (GPCR) GTPases and cell signaling and cycling associated guanine nucleotide exhange factors (GEF).

  12. ATR inhibitor

    Camonsertib is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. 

  13. RAD51 inhibitor

    Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain.
  14. HDAC1 and HDAC3 inhibitor

    Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively.
  15. fluorescent probe

    DAPI Dihydrochloride is a cell-permeable fluorescent probe used to stain DNA and chromosomes, with a preference for adenine and thymine rich DNA.
  16. broad-spectrum seed treatment nematicide

    Tioxazafen is a disubstituted oxadiazole and a broad-spectrum seed treatment nematicide. Tioxazafen is designed to provide consistent broad-spectrum control of nematodes in corn, soy, and cotton.
  17. EG1

    Pax2 inhibitor

    EG1 is a specific Paired box 2 (Pax2) inhibitor that targets the DNA binding domain and inhibits embryonic kidney development.
  18. SIRT1/SIRT3 inhibitor

    4'-bromo-Resveratrol is a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3).

  19. DNA alkylator

    Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent.
  20. ADCs cytotoxin

    PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin.
  21. DNA gyrase/topoisomerase inhibitor

    Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor.
  22. DHPS inhibitor

    GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor.
  23. topoisomerase I inhibitor

    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
  24. FIPV inhibitor

    GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM.
  25. tankyrase 1/2 inhibitor

    G244-LM is a potent and specific tankyrase 1/2 inhibitor that inhibits Wnt signaling.
  26. HDAC2 inhibitor

    BRD6688 is a selective inhibitor of HDAC2 that acts by enhancing the learning and memory processes.
  27. polymerase inhibitor

    ERDRP-0519 is an orally available inhibitor of polymerase that shows efficacy against a lethal morbillivirus infection in a large animal model.
  28. ATR inhibitor

    Gartisertib (VX-803, ATR inhibitor 2) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM.

  29. Topoisomerase agonist

    Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR).
  30. NAD+ competitive inhibitor of PARP7

    RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM).
  31. DNA replication inhibitor

    Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator.
  32. anticancer agent

    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  33. HDAC3 inhibitor

    BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM.
  34. HDAC6 inhibitor

    Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM.
  35. antidepressant agent

    Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
  36. telomerase activation agent

    Astramembrangenin (Cycloastragenol) is a compound isolated from the roots of Astragalus kuhitangi (Nevski) Sirj.
  37. pan-HDAC inhibitor

    Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.
  38. topoisomerase I inhibitor

    Topovale, also known as ARC-111, is a potent topoisomerase I inhibitor.
  39. ARTD10 (PARP-10) inbitor

    OUL35, also known as NSC39047, is a selective PARP-10 inhibitor, and small-molecule ARTD10 inhibitor.
  40. Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a novel lipid acyclic nucleoside phosphonate that delivers high intracellular concentrations of the active antiviral agent tenofovir.
  41. Riamilovir, also known as Triazavirin, is a nucleoside analogue of nucleic acid and an antiviral agent, works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture.
  42. eIF4A Inhibitor

    Zotatifin is a highly selective inhibitor of eIF4A, targeting the assembly of the eIF4F initiation complex. With an IC50 of 2 nM, it promotes eIF4A binding to specific mRNA recognition motifs in the 5’-UTRs. Zotatifin exhibits significant antiviral properties, effectively reducing the infectivity of SARS-CoV-2 by inhibiting the biogenesis of its NP protein (IC90 = 37 nM) and also induces apoptosis in cancer cells. This compound is valuable for studies related to viral infections and translational control mechanisms.
  43. Fluorometric HDAC Substrate

    Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors.
  44. PARP1 Degrader

    iRucaparib-AP6 is a potent PROTAC compound that selectively targets PARP1 for degradation. This non-trapping degrader inhibits both the catalytic activity and scaffolding functions of PARP1, effectively disrupting its role in DNA repair pathways. iRucaparib-AP6 is useful in studying the biology of PARP1 and its implications in cancer research, particularly in understanding resistance mechanisms to PARP inhibitors.
  45. VUBI1 Analogue

    VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies.
  46. PROTAC PARP1 Degrader

    PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein.
  47. RNA RIBOTAC Degrader

    Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology.
  48. SIRT2 Inhibitor

    SIRT2-IN-8 is a selective inhibitor of SIRT2 (Sirtuin 2), a member of the sirtuin family of proteins implicated in various cellular processes. This compound exhibits strong inhibition of SIRT2 activity, making it a valuable tool for investigating the role of SIRT2 in neurodegenerative diseases, particularly Huntington's and Parkinson's diseases. Its use in research can contribute to a better understanding of the molecular mechanisms underlying these conditions and aid in the development of therapeutic strategies.
  49. HDAC Inhibitor

    HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression.
  50. HIV Reverse Transcriptase Inhibitor

    β-Rubromycin is a selective inhibitor of HIV-1 reverse transcriptase, exhibiting a Ki of 0.27 μM. Additionally, it demonstrates potent telomerase inhibition with an IC50 of 3 μM. β-Rubromycin effectively inhibits the proliferation of K-562 and HeLa cell lines, showing IC50 values of 19.5 µM and 22.7 µM, respectively, making it a valuable tool for research in HIV and telomerase-related studies.

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