DNA Damage

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  1. PARP inhibitor

    AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.
  2. Alendronate is a nitrogen-containing bisphosphonate that is commonly used in the treatment of osteoporosis and other metabolic bone diseases.
  3. DNA/RNA Synthesis inhibitor

    Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.
  4. HDAC inhibitor

    JNJ-26481585 (Quisinostat) is a pan-HDAC inhibitor with marked potency toward HDAC1 (IC(50), 0.16 nmol/L).
  5. HDAC Inhibitor

    LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma.
  6. HDAC Inhibitor

    Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.
  7. DNA, RNA Synthesis Inhibitor

    CCT239065 is a mutant protein kinase inhibitor that inhibits signaling downstream of V600EBRAF in cancer cells, blocking DNA synthesis, and inhibiting proliferation.
  8. mTOR inhibitor

    Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).
  9. Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNA damage agent.
  10. DNA-PK inhibitor

    Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM).
  11. HDAC inhibitor

    Romidepsin strongly inhibits HDAC1 and HDAC2 with IC5N/A of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC5N/A 25 nM and 79N/A nM, respectively.
  12. HDAC inhibitor

    Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
  13. Sirtuin-1 (SIRT1) activator

    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  14. eIF4E-eIF4G interaction inhibitor

    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  15. HDAC1/HDAC2 inhibitor

    BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50=?1 and 8 nM), extracted from patent US2018360927.
  16. HDAC inhibitor

    Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II. It binds to and inhibits HDACs leading to an accumulation of highly acetylated histones.
  17. HDAC4 inhibitor

    Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.
  18. Topoisomerase II inhibitor

    Amrubicin is a synthetic anthracycline antibiotic. It inhibits DNA topoisomerase II. Antineoplastic.
  19. Palifosfamide is a synthetic mustard compound with potential antineoplastic activity.
  20. HDAC inhibitor

    Apicidin is a a potent histone deacetylases (HDAC) inhibitor with potential anticancer activity.
  21. HDAC6 inhibitor

    ACY-241 is a new, selective and orally available inhibitor of HDAC6.
  22. SIRT2 inhibitor

    AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).
  23. HDAC6 inhibitor

    BRD9757 is a highly potent and selective HDAC6 inhibitor with an IC50 of 30 nM toward HDAC6.
  24. Topoisomerase II inhibitor

    Pixantrone is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  25. modified nucleoside

    6-O-Methyl Guanosine is a modified nucleoside. 6-O-Methyl Guanosine (6-methylguanosine) inhibit colony-forming ability in a malignant xeroderma pigmentosum cell line.
  26. topoisomerase 1 inhibitor

    Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity.
  27. DNA-PK inhibitor

    KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency.
  28. 1,3-β-D-glucan synthase inhibitor

    Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.
  29. biomarker

    N6-Etheno 2'-deoxyadenosine is a reactive oxygen species (ROS)/reactive nitrogen species (RNS)-induced DNA oxidation product, used as a biomarker to evaluate chronic inflammation and lipid peroxidation in animal or human tissues.
  30. ATR inhibitor

    ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
  31. 3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer.
  32. JAK2/HDAC dual inhibitor

    JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines.
  33. Topo II inhibitor

    BNS-22 is a potent small molecule inhibitor of Topo II (IC50 2.8 M and 0.42 M for Topo II alpha and Topo II beta, respectively).
  34. IMPDH inhibitor

    AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).

  35. 3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.
  36. DNA topoisomerase II inhibitor

    Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
  37. IRE1α inhibitor

    APY29 inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
  38. topoisomerase I/II inhibitor

    TAS 103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models
  39. Topoisomerase II inhibitor

    Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication
  40. eIF4E/eIF4G inhibitor

    4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.
  41. SIRT2 inhibitor

    AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.
  42. DNA/RNA Synthesis inhibitor

    Chlorambucil is a nitrogen mustard alkylating agent.
  43. MTH1 (NUDT1) inhibitor

    (S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM.
  44. PERK inhibitor

    ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.
  45. HDAC inhibitor

    TMP195 is the most potent and selective class IIa HDAC inhibitor.
  46. HDAC inhibitor

    4SC-202 is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity.
  47. Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. It acts by induction of DNA strand breaks.
  48. APE1 Redox Inhibitor

    E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
  49. Ack1 (TNK2) inhibitor

    AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.

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