DNA Damage

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Product Citation
  1. PI3K Inhibitor

    PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 μM and 1.3 μM, respectively.
  2. Topoisomerase II inhibitor

    Pirarubicin is an analogue of the anthracycline anti-neoplastic doxorubicin. Intercalates into DNA and interacts with Topo II (topoisomerase II) and supressing DNA replication
  3. HDAC Inhibitor

    Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent.
  4. DNA/RNA Synthesis inhibitor

    Raltitrexed (Tomudex) is an inhibitor of thymidylate synthase and also is one of the strongest antimetabolites in use.
  5. RNA polymerase inhibitor

    Rifabutin is a bactericidal antibiotic drug primarily used in the treatment of tuberculosis. Its effect is based on blocking the DNA-dependent RNA-polymerase of the bacteria.
  6. RNA polymerase inhibitor

    Antibiotic; inhibits bacterial RNA polymerase. Prototypical activator of the pregnane X receptor (PXR).
  7. 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.
  8. HDAC inhibitor

    Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).
  9. HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) 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.
  10. 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.
  11. DNA topoisomerase I inhibitor

    Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor.
  12. HDAC Inhibitor

    Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.
  13. HDAC6 inhibitor

    Tubacin (tubulin acetylation inducer) is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM.
  14. HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
  15. PARP inhibitor

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

    AR-42 is a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit.
  17. 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).
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. Transcriptase inhibitor

    Abacavir is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
  23. Transcriptase inhibitor

    Abacavir sulfate is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
  24. 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.
  25. HDAC inhibitor

    PCI-34051 is a specific and potent histone deacetylase 8 (HDAC8) inhibitor, with >200-fold selectivity over the other HDAC isoforms.
  26. 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.
  27. PI3K inhibitor

    Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

  28. MDMX Inhibitor

    NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.

  29. Topoisomerase I inhibitor

    Exatecan inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death.
  30. PARP inhibitor

    BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
  31. HDAC inhibitor

    M344 is a potent inhibitor of HDAC with IC50 of 100 nM and able to induce cell differentiation.
  32. HDAC inhibitor

    BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 μM, respectively).
  33. DNA synthesis inhibitor

    Gemcitabine (LY 188011) is a DNA synthesis inhibitor which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.
  34. TNKS inhibitor

    TC-E 5001 is dual tankyrase (TNKS) inhibitor (Kd values are 79 and 28 nM for TNKS1 and TNKS2 respectively, IC50 = 33 nM for TNKS2) that is devoid of activity at PARP1 and PARP2 (IC50 >19 uM). Inhibits Wnt signaling and stabilizes Axin2 levels.
  35. MPGES-1 inhibitor

    MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively.
  36. DNA synthesis inhibitor

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

    Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.
  38. eIF4A inhibitor

    Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis.
  39. 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).
  40. 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.

  41. ATM/ATR inhibitor

    VE-821 is a potent and selective inhibitor of protein kinase ATR.
  42. RHA inhibitor

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

    Balofloxacin is a quinolone antibiotic. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae.
  44. Topoisomerase inhibitor

    Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase).
  45. 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).
  46. Topoisomerase II inhibitor

    Flumequine is a synthetic chemotherapeutic antibiotic which affecting mammalian chromosome and DNA unwinding at the level of gyrase/topoisomerases.
  47. 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.
  48. HDAC6 inhibitor

    ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation.
  49. HDAC Inhibitor

    CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells.
  50. Topoisomerase

    (S)-10-Hydroxycamptothecin is a camptothecin derivative that inhibits DNA topoisomerase by enacting strand breaks in chromosomal DNA and inducing apoptosis.

Items 51-100 of 419

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