Proteases

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Items 351-400 of 1109

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  1. synthetic thrombin inhibitor

    OM-189 is a selective synthetic thrombin inhibitor.
  2. MMP-13 inhibitor

    DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity.
  3. TNAP inhibitor

    SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
  4. MMP inhibitor

    BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  5. Phosphatase inhibitor

    Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity.
  6. KGA inhibitor

    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM.
  7. uPA inhibitor

    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively.
  8. DPP8/9 inhibitor

    1G244 is a novel potent and selective DPP8/9 inhibitor.
  9. DHODH inhibitor

    BRD9185 is a Dihydroorotate dehydrogenase (DHODH) inhibitor.
  10. INH inhibitor

    INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.
  11. proteasome β1i (LMP2) subunit inhibitor

    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
  12. HIV capsid inhibitor

    CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
  13. GAC inhibitor

    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  14. PPP1R15B inhibitor

    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B).
  15. Thrombin inhibitor

    Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin.
  16. HIV infection inhibitor

    HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
  17. Cysteine protease inhibitor

    LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
  18. PME-1 inhibitor

    ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
  19. LMP2 inhibitor

    KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
  20. CDC25 phosphatase family inhibitor

    BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family.
  21. ecto-ATPase inhibitor

    ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively.
  22. alpains 1 and 2 inhibitor

    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
  23. 20S proteasome inhibitor

    Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity.
  24. Calpain Inhibitor

    Calpain Inhibitor II, ALLM is a cell-permeable inhibitor of calpain I, calpain II, cathepsin L and cathepsin B with Ki values of 120 nM, 230 nM, 0.6 nM and 100 nM, respectively.
  25. HLE inhibitor

    Elastase Inhibitor, SPCK is a potent, irreversible inhibitor of human leukocyte elastase (HLE) (Ki = 10 uM).
  26. Caspase inhibitor

    Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity.
  27. Caspase-3/7 Inhibitor

    MMPSI is a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM).

  28. 20S proteasome inhibitor

    AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins.
  29. Proteasome inhibitor

    Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent.
  30. Reversible thrombin inhibitor

    Bivalirudin is a synthetic 20 residue peptide which reversibly inhibits thrombin.
  31. HIV-1 attachment inhibitor

    BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.
  32. CPG2 inhibitor

    Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
  33. direct thrombin inhibitor

    Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.
  34. thrombin inhibitor

    Dabigatran ethyl ester, which is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity.
  35. HIV protease inhibitor

    Fosamprenavir Calcium Salt is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.
  36. HCV Protease inhibitor

    MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
  37. HCV Protease inhibitor

    MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
  38. HCV Protease inhibitor

    MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
  39. HCV replication inhibitor

    RO-9187 is a potent inhibitor of HCV virus replication in the replicon system (IC(50) = 171 +/- 12 nM; CC(50) >1 mM).
  40. DPP-4 inhibitor

    Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
  41. HIV protease inhibitor

    Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates.
  42. Selective calpain inhibitor

    Acetyl-Calpastatin (184-210) (human), selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 uM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.
  43. MMP-2 inhibitor

    ARP 101, selective inhibitor of MMP-2 that displays ~ 600-fold selectivity over MMP-1 (IC50 values are 0.81 and 486 nM respectively).
  44. Caspase-3 inhibitor

    AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 uM).
  45. Calpain inhibitor

    Calpeptin is a cell permeable calpain inhibitor.
  46. MMP inhibitor

    CP 471474, broad spectrum MMP inhibitor (IC50 values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively).
  47. DPP-4 inhibitor

    DPPI 1c hydrochloride is a dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of CD26 (DPP 4), with an IC50 = 106 nM and little activity against DPP II, DPP III, DPP VIII, DPP IX, FAP, or APP even at concentrations as high as 30 μM.
  48. Aminopeptidase inhibitor

    Fumagillin is a complex natural product antibiotic which covalently binds a key histidine residue of methionine aminopeptidase type II (MetAP-2), inhibiting endothelial cell proliferation and angiogenesis.
  49. γ-secretase inhibitor

    JLK 6 is an inhibitor of γ-secretase that selectively inhibits APP cleavage without affecting other γ-secretase-mediated pathways.
  50. Cathepsin K Inhibitor

    L006235 is a potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S.

Items 351-400 of 1109

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