DNA Damage

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  1. HDAC/ER stress inhibitor

    Sodium phenylbutyrate is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
  2. IRE1α inhibitor

    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  3. HDAC6 inhibitor

    Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  4. ATM inhibitor

    AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
  5. ATM inhibitor

    AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
  6. ATM inhibitor

    AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
  7. Topoisomerase inhibitor

    Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
  8. 4EBP1 inhibitor

    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  9. HDAC inhibitor

    SR-4370 is an HDAC inhibitor. SR-4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp.
  10. topoisomerase IV inhibitor

    Ciprofloxacin hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, an fluoroquinolone antibiotic that is widely used as an antimicrobial and immunomodulatory agent
  11. PARP agonist

    Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.
  12. Ethynylcytidine is a synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities.
  13. SIRT 6 inhibitor

    OSS-128167, also known as SIRT6-IN-1, is a potent and selective SIRT 6 inhibitor with IC50 value of 89 μM.
  14. DNA-PK inhibitor

    Nedisertib, also known as M-3814, MSC2490484A, is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities.
  15. PARP inhibitor

    Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. CAS: 1446261-44-1 (free base) 2086689-94-1 (maleate) 2086689-93-0 (hydrate)
  16. HDAC8 inhibitor

    HDAC8-IN-1, is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines.
  17. Azoxymethane is a colon carcinogen which leads to the formation of DNA adducts.
  18. TNK2 inhibitor

    XMD16-5 is a tyrosine kinase nonreceptor 2(TNK2) inhibitor.
  19. TNK2 Inhibitor

    XMD8-87 is an inhibitor of tyrosine kinase non-receptor 2 (TNK2) with an IC50 value of 1.9 μM
  20. NHEJ inhibitor

    SCR7 pyrazine is an inhibitor of nonhomologous end-joining (NHEJ).
  21. SIRT3 inhibitor

    3-TYP is a SIRT3 inhibitor.
  22. SIRT2 inhibitor

    Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
  23. GARFT inhibitor

    Pelitrexol is a GARFT inhibitor, and is also a water soluble antifolate with anti-proliferative activity.
  24. SIRT6 allosteric activator

    MDL-800 is a first-in-class cellularly active SIRT6 allosteric activator.
  25. Sulfamonmethoxine is a competitive inhibitor of dihydropteroate synthetase, blocking the synthesis of folic acid.
  26. DNA/RNA Alkylator

    Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
  27. 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.
  28. Procaine hydrochloride is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
  29. Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics with activity similar to oxolinic acid and nalidixic acid.
  30. Anthralin, also known as Dithranol, is a hepsin activity inhibitor used for treatment of psoriasis Inhibition of hepsin activity suppresses the invasive growth of the tumor. Anthralin exerts a direct effect on keratinocytes and leukocytes. Anthralin significantly prolonged the prophase of mitotic keratinocytes in subtoxic doses and suppressed the expression of keratin 6 mRNA in the immediately suprabasal layer of psoriatic epidermis in vivo. Anthralin also inhibits the transformation of lymphocytes and the release of reactive oxygen species from activated leukocytes, in vitro.
  31. nucleoside

    Thymidine is a nucleoside in which THYMINE is linked to DEOXYRIBOSE. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.

  32. Clevudine is an antiviral drug for the treatment of hepatitis B.
  33. Topoisomerase IV inhibitor

    Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.
  34. Nimustine hydrochloride is an antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine.
  35. nucleoside analog

    Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM.
  36. topoisomerase II inhibitor

    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
  37. topoisomerase IIα inhibitor

    Dexrazoxane is an intracellular iron chelator and an inhibitor of topoisomerase IIα.
  38. HDAC inhibitor

    Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
  39. antifolate agent

    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
  40. Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm.
  41. PARP inhibitor

    Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1, and also shows binding affinity to eight other PARP domains.
  42. PARP1 and PARP2 inhibitor

    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
  43. Topoisomerase I inhibitor

    Belotecan, also known as CKD-602, is the semi-synthetic camptothecin analogue belotecan with potential antitumor activity.
  44. topoisomerase II inhibitor

    Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
  45. Gemifloxacin Mesylate is a third generation antibacterial quinolone agent that is also fluorinated.
  46. PARG inhibitor

    Ethacridine lactate is a topically applied anti-infective agent. Ethacridine lactate is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
  47. Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
  48. Treosulfan (NSC 39069;Treosulphan) is an alkylating agent with activity in ovarian cancer and other solid tumor types.
  49. HDAC6 inhibitor

    SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.
  50. HDAC inhibitor

    EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.

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