DNA Damage

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  1. DNA/RNA Synthesis inhibitor

    Cidofovir (Vistide) is an antiviral used for the treatment of cytomegalovirus (CMV) infection (ie: retinitis).
  2. DNA topoisomerase Inhibitor

    SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor).
  3. PARP inhibitor

    AG-014699 (Rucaparib) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.
  4. eIF4E/eIF4G inhibitor

    4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.
  5. DNA/RNA Synthesis inhibitor

    Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.
  6. HDAC6 inhibitor

    ACY-241 is a new, selective and orally available inhibitor of HDAC6.
  7. Topoisomerase II inhibitor

    Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.
  8. IRE1α inhibitor

    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  9. PI3K/HDAC inhibitor

    CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.
  10. DNA-PK inhibitor

    NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.
  11. DNA-PK inhibitor

    NU7026 is a novel DNA-dependent protein kinase inhibitor that potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.
  12. HDAC Inhibitor

    MC1568 is a member of HDAC inhibitors that inhibits the histone deacetylase class II by modifying the genetic expression of various important genes of cell cycle mostly at G1 phase, resulting in the death of breast cancer cells by apoptosis.
  13. DNA/RNA Synthesis inhibitor

    Daptomycin is a lipopeptide antibiotic used in the treatment of certain infections caused by Gram-positive organisms.
  14. DNA topoisomerase II inhibitor

    Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
  15. DNA/RNA Synthesis inhibitor

    Gemcitabine (Gemzar) is a newer chemotherapy drug acting by replacing one of the building blocks of nucleic acids during DNA replication in cancer cells, preventing tumor growth.
  16. RHA inhibitor

    YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.
  17. 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.
  18. HDAC inhibitor

    Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  19. HDAC6 inhibitor

    ACY-738 is a potent and selective HDAC6 inhibitor with improved brain bioavailability. ACY-738 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs.
  20. HDAC Inhibitor

    LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma.
  21. 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).
  22. PI3K Inhibitor

    PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.
  23. TNKS inhibitor

    G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice,
  24. viral RNA polymerase inhibitor

    T-705, a substituted pyrazine compound, has been found to exhibit potent anti-influenza virus activity in vitro and in vivo.

  25. ATM Inhibitor

    KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.
  26. HDAC inhibitor

    ITF2357 (Givinostat) is a HDACs inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.
  27. ATR inhibitor

    ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
  28. IRE1 Rnase inhibitor

    4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
  29. HDAC inhibitor

    SB939 is an oral inhibitor of HDAC, selective for class I, II and IV HDACs and displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay.
  30. eIF2α dephosphorylation inhibitor

    Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).
  31. DNA/RNA Synthesis inhibitor

    CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively

  32. HCV Polymerase Inhibitor

    VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent polymerase with sub-micromolar IC50 values versus genotype 1a/1b replicons.
  33. Topoisomerase inhibitor

    Moxifloxacin is a quinolone/fluoroquinolone antibiotic.
  34. Telomerase Inhibitor

    BIBR 1532 is a selective telomerase inhibitor (IC50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively).

  35. HDAC6 inhibitor

    CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
  36. HDAC6 inhibitor

    Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
  37. HDAC Inhibitor

    LBH589 is a hydroxamic acid and acts as a non-selective HDAC inhibitor with IC5o of HDAC1 to be 0.23 nM.
  38. PARP-1 inhibitor

    Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells.
  39. PARP1 inhibitor

    BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.
  40. Topoisomerase inhibitor

    Irinotecan (CPT 11), a compound within the camptothecin family, is an inhibitor of topoisomerase 1 involved in cellular DNA replication and transcription.
  41. DNA synthesis inhibitor

    Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.
  42. PARP inhibitor

    MK-4827 is a novel potent, orally bioavailable PARP-1 and PARP-2 inhibitor.
  43. ATR inhibitor

    Berzosertib (VE-822) is an potent ATR inhibitor.

     
  44. ATR inhibitor

    BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
  45. ATR inhibitor

    AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.
  46. RNA polymerase inhibitor

    BMH-21 is a potent small molecule DNA intercalator. BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
  47. PARP Inhibitor

    3-Aminobenzamide is a novel PARP inhibitor, known to sensitize cells to radiation in vitro by inhibiting the repair of DNA damage.
  48. 1,3-β-D-glucan synthase inhibitor

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

    PCI-24781 is a broad-spectrum phenyl hydroxamic acid HDAC inhibitor.
  50. Topoisomerase I inhibitor

    Camptothecin is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I).

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