Proteases

Items 151-200 of 1366

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  1. PP2A inhibitor

    Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM.
  2. HIV protease inhibitor

    Darunavir Ethanolate (Prezista) is an HIV protease inhibitor.
  3. Indinavir sulfate is a novel hydroxyaminopentane amide class of HIV-1 protease inhibitors.
  4. Apoptosis Activator

    Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells
  5. Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
  6. Cathepsin K inhibitor

    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys.
  7. HCV NS3/4A protease inhibitor

    Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of NS3/4A protease polymorphisms. GS-9857 improves coverage against commonly encountered NS3 resistance-associated variants (RAVs).
  8. thrombin/factor Xa dual inhibitor

    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  9. NF-kB inhibitor/Proteasome activator

    18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1).
  10. Proteasome inhibitor

    MG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome.
  11. transglutaminase 2 (TG2) inhibitor

    ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, which can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD).
  12. proteasome inhibitor

    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
  13. IMPase inhibitor

    L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively.
  14. MTP inhibitor

    PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.

  15. Proteasome inhibitor

    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  16. Caspase/apoptosis activator

    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  17. DHODH inhibitor

    ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models.

  18. cathepsin S inhibitor

    Petesicatib is a cathepsin S inhibitor, used in research of immune diseases.
  19. FABP4 Inhibitor is a cell-permeable biphenylazolo-oxyacetate that acts as a potent and selective inhibitor of adipocyte Fatty-Acid-Binding Protein (aFABP/aP2) by targeting its fatty acid-binding pocket (Ki = < 2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP's (Ki = 250 nM and 350 nM, respectively).
  20. HCV NS5B polymerase inhibitor

    Deleobuvir (BI207127) was a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C

  21. 4-Butylresorcinol is a phenol derivative which can inhibit tyrosinase with IC50 of 11.27 μM.
  22. aldose reductase inhibitor

    Ranirestat is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy.
  23. HCV NS3 inhibitor

    GS-9451 is a potent macrocyclic HCV NS3 PI that achieved a median maximal change in HCV RNA of 3.6 log10 IU/mL (range, -4.7 log10 to -3.1 log10 IU/mL) following 3-day monotherapy in treatment-nave patients with HCV genotype 1 infection during phase I.
  24. DPP-4 inhibitor

    Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.
  25. FABP inhibitor

    HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
  26. DPP-4 inhibitor

    Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.
  27. Aminopeptidase inhibitor

    Bestatin methyl ester is a cell-permeable derivative of Bestatin which displays slightly stronger inhibition of neutral aminopeptidase than Bestatin, but has much weaker activity against basic aminopeptidase.
  28. MMP-13 inhibitor

    CL-82198 is a selective inhibitor of human collagenase-3, also known as matrix metalloproteinase-13 (MMP-13), producing 89% inhibition at 10 mg/ml.
  29. HIV protease inhibitor

    PNU-103017 is an HIV protease inhibitor.
  30. Serine protease inhibitor

    AAF-CMK is a serine protease inhibitor which irreversibly inhibits TPPII (tripeptidyl peptidase II), a giant protease which may substitute for some proteasome functions1, and reversibly inhibits Cln2 (TPPI).
  31. cathepsin C substrate

    Gly-Phe-beta-naphthylamide is a cathepsin C substrate. The compound is described to accumulate inside lysosomes leading to their destruction.
  32. reversible Calpain inhibitor

    SJA6017 is a cell permeable peptide aldehyde which functions as a reversible calpain inhibitor.
  33. Proteasome inhibitor?€?

    VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3uM).
  34. gamma-secretase inhibitor

    Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID).
  35. SPPL2a inhibitor

    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
  36. neprilysin inhibitor

    AHU-377 is an inhibitor of neprilysin with IC50 value of 5nM.
  37. 25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types
  38. 20S proteasome inhibitor

    Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi.
  39. neprilysin (NEP) inhibitor

    TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.
  40. TACE/MMP inhibitor

    (S,S)-TAPI-0 is an inhibitor of TACE (IC50 = 50-100 nM) as well as other matrix and membrane metalloproteases

  41. DPIV and DP8/9 inhibitor

    DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
  42. HCV NS3/4a inhibitor

    MK-5172 is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
  43. Hec1 imhibitor

    INH1 is a Hec1 inhibitor. It binds Hec1, inhibiting its association with Nek2 and kinetochores.
  44. NEP inhibitor

    LHW090-A7 is an inhibitor of neutral endopeptidase (NEP), an enzyme responsible for the metabolic inactivation of enkephalins.
  45. nucleotide analog HCV inhibitor

    PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.
  46. HCV NS5A inhibitor

    MK 8742, also known as Elbasvir, is a HCV NS5A inhibitor, which is an all-oral, interferon-free regimen for the treatment of HCV infection.
  47. TACE/MMP inhibitor

    TAPI-2 is an inhibitor of TACE, ADAMs, ACE secretase, and other MMPs (metalloproteinases). TAPI-2 blocks release of DCC7, APP, TNFα, L-selectin, NOTCH, TGFα, IL-6R9, erbB2/HER2, and ACE. This inhibitor has been used in tissue culture.
  48. HCV NS3/4A protease inhibitor

    GS-9451, a novel hepatitis C virus (HCV) nonstructural 3/4a (NS3/4a) protease inhibitor, is highly active in patients infected with HCV genotype 1 (GT 1).
  49. PSI

    Proteasome inhibitor

    PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome.
  50. TACE/MMP inhibitor

    TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors.

Items 151-200 of 1366

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