DNA Damage

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  1. RSV polymerase inhibitor

    ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
  2. DNA-PK inhibitor

    (Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM.
  3. non-nucleoside inhibitor

    Filibuvir is a potent, selective non-nucleoside inhibitor (NNI) of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase, and it binds noncovalently in the ??Thumb 2?? pocket of NS5B.
  4. flaviviruse inhibitor

    NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM.
  5. gyrase B inhibitor

    VXc-486 is a gyrase B inhibitor, with bactericidal activity.
  6. HDAC inhibitor

    Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
  7. HCV NS5B RNA-dependent RNA polymerase inhibitor

    Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
  8. SIRT2 inhibitor

    JFD00244 is a sirtuin 2 (SIRT2) inhibitor. Anti-tumor effect.
  9. IRE1 RNase inhibitor

    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29?μM in human vitro.
  10. HDAC5/HDAC9 inhibitor

    BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
  11. GlyRS inhibitor

    GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
  12. F1/FO-ATP synthase complex inhibitor

    ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.
  13. LRS inhibitor

    Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation.
  14. HDAC11 inhibitor

    FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
  15. HDAC1 /HDAC2 inhibitor

    ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.
  16. DNA polymerase-beta inhibitor

    5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
  17. PARP14 inhibitor

    GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 ?M.
  18. GCN2 inhibitor

    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
  19. SIRT5 inhibitor

    SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
  20. HDAC6/8/10 inhibitor

    TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.
  21. ATR inhibitor

    ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 ?μ.
  22. BRD4 inhibitor

    CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 .
  23. ATM inhibitor

    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM.
  24. HDAC6 inhibitor

    ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms.
  25. DNA-PK inhibitor

    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  26. DNA-PK inhibitor

    AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumor activity.
  27. Sirt2 inhibitor

    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.
  28. HDAC/proteasome inhibitor

    RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
  29. DNA topoisomerase I/II inhibitor

    Intoplicine is a DNA topoisomerase I and II inhibitor.
  30. telomerase inhibitor

    TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
  31. NS5B polymerase inhibitor

    ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
  32. PARP-2 inhibitor

    PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
  33. arginyl tRNA synthetase inhibitor

    Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
  34. pan HDAC inhibitor

    Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
  35. AARS inhibitor

    Gln-AMS is an aminoacyl-tRNA synthetases (AARS) inhibitor, which binds the A-domain within the NRPS enzymes.
  36. HDAC inhibitor

    Oxamflatin (Metacept-3) is a potent HDAC inhibitor with an IC50 of 15.7 nM.
  37. aspartyl-tRNA synthetase inhibitor

    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  38. PARG inhibitor

    PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.
  39. IRE-1 RNase inhibitor

    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
  40. GCN2 inhibitor

    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  41. HDAC6 inhibitor

    WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
  42. BRCA1 inhibitor

    BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.
  43. PPI inhibitor

    BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
  44. PDI inhibitor

    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively.
  45. RNA polymerase inhibitor

    Pseudouridimycin (PUM), an antibiotic, is a selective bacterial RNA polymerase (RNAP) inhibitor. Pseudouridimycin is a C-nucleoside analogue that is effective against both Gram-negative and Gram-positive bacteria.
  46. DNA polymerase IIIC inhibitor

    ACX-362E is an orally available DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E displays very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens.
  47. cNIIIB nucleotidase inhibitor

    7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor with IC50 value of 87.8????7.5??M.
  48. PNP inhibitor

    CI 972 is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (Ki=0.83 μM) under development as a T cell-selective immunosuppressive agent.
  49. OPRTase inhibitor

    Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase[1]. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 ?M in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
  50. PARP14 inhibitor

    PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (??24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.

Items 251-300 of 1503

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