DNA Damage

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Product Name
Application
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Product Citation
  1. 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.
  2. HDAC inhibitor

    PCI-34051 is a specific and potent histone deacetylase 8 (HDAC8) inhibitor, with >200-fold selectivity over the other HDAC isoforms.
  3. 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.
  4. 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).

  5. 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.

  6. 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.
  7. PARP inhibitor

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

    M344 is a potent inhibitor of HDAC with IC50 of 100 nM and able to induce cell differentiation.
  9. 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).
  10. 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.
  11. 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.
  12. 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.
  13. DNA synthesis inhibitor

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

    Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.
  15. 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.
  16. Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
  17. 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).
  18. 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.

  19. Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii.
  20. ATM/ATR inhibitor

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

    YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.
  22. Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
  23. Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
  24. Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNA damage agent.
  25. Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
  26. 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.
  27. Topoisomerase inhibitor

    Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase).
  28. 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).
  29. Azithromycin is an azalide antibiotic, which inhibits the growth of gram negative bacteria, such as Haemophilus influenza.
  30. Adenine sulfate is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
  31. Topoisomerase II inhibitor

    Flumequine is a synthetic chemotherapeutic antibiotic which affecting mammalian chromosome and DNA unwinding at the level of gyrase/topoisomerases.
  32. Pefloxacin mesylate is a synthetic chemotherapeutic agent and an antibacterial agent with IC5N/A of 6.7 nM.
  33. 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.
  34. 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.
  35. HDAC Inhibitor

    CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells.
  36. Schisandrin B is the most abundant dibenzocyclooctadiene isolated from the fruit of Schisandra chinensis (Turcz) Baillon or Wu-Wei-Zi (transliterally meaning "the fruit of five tastes" in Chinese), which is a commonly used tonic herb in Chinese medicine, particularly for the treatment of liver ailments.
  37. Topoisomerase

    (S)-10-Hydroxycamptothecin is a camptothecin derivative that inhibits DNA topoisomerase by enacting strand breaks in chromosomal DNA and inducing apoptosis.
  38. Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties.
  39. DNA topoisomerase Inhibitor

    SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor).
  40. 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.
  41. 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.
  42. HDAC inhibitor

    CRA-026440 is a potent, broad-spectrum HDAC inhibitor.
  43. sirtuin inhibitor

    Sirtinol is a cell-permeable, specific inhibitor of sirtuin NAD-dependant histone deacetylases. It is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
  44. HDAC inhibitor

    CXD101 is a class I-selective HDAC inhibitor (HDAC1 (IC50, 63 nM), HDAC2 (IC50, 570 nM), HDAC3 (IC50, 550 nM). CXD101 has no activity against HDAC class II.
  45. Sirt1/Sirt2 inhibitor

    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  46. p53 activator

    Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.
  47. Aldoxorubicin, also known as INNO-206, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity.
  48. eIF4E-eIF4G interaction inhibitor

    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  49. SIRT1/SIRT2 inhibitor

    Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.
  50. PARP Inhibitor

    AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein.

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