Proteases

Items 101-150 of 1366

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  1. HCV RNA polymerase inhibitor

    PSI-6206 is the deaminated derivative of PSI-6130, which is a potent inhibitor of hepatitis C virus (HCV) replication in the subgenomic HCV reolicon system.
  2. HCV NS5B polymerase inhibitor

    Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
  3. HCV replication inhibitor

    R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).
  4. HIV Protease Inhibitor

    Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
  5. HCV NS3/4A protease inhibitor

    Simeprevir is a potent inhibitor of HCV NS3/4A protease (Ki = 0.36 nM) and viral replication (replicon EC50 = 7.8 nM).
  6. NS5B polymerase inhibitor

    Tegobuvir (GS-9190 is a non-nucleoside NS5B polymerase inhibitor.
  7. PP2A inhibitor

    LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
  8. HCV NS3/4A protease inhibitor

    Vaniprevir is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
  9. Reversible Proteasome Inhibitor

    MG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis.
  10. aldose reductase inhibitor

    Epalrestat is an aldose reductase inhibitor.
  11. Camostat mesylate is an orally active protease inhibitor. Known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin.
  12. Thrombin inhibitor

    Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.
  13. Aldose reductase inhibitor

    Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.
  14. 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.
  15. HIV protease inhibitor

    Darunavir Ethanolate (Prezista) is an HIV protease inhibitor.
  16. Indinavir sulfate is a novel hydroxyaminopentane amide class of HIV-1 protease inhibitors.
  17. 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
  18. 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)
  19. Cathepsin K inhibitor

    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys.
  20. 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).
  21. 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.
  22. 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).
  23. Proteasome inhibitor

    MG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome.
  24. 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).
  25. proteasome inhibitor

    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
  26. 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.
  27. MTP inhibitor

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

  28. Proteasome inhibitor

    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  29. 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.
  30. MMP9 inhibitor

    JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
  31. γ-Secretase Modulator

    NGP-555 is a gamma-secretase modulator with a selective mechanism to reduce Abeta 42 while raising shorter Abeta forms such as Abeta 37 and 38.
  32. DHODH inhibitor

    DSM265 is a long-duration, potent and selective dihydroorotate dehydrogenase (DHODH)) inhibitor.
  33. DUSP26 inhibitor

    F1063-0967 is a novel inhibitor of dual-specificity phosphatase 26 (DUSP26), inducing apoptosis in IMR-32 cell line.
  34. DPPI inhibitor

    AZD7986, also known as INS 1007, is a second generation reversible covalent, potent and selective DPP1 inhibitor potentially for the treatment of chronic obstructive pulmonary disease (COPD) with predicted human PK properties suitable for once daily human dosing.
  35. TNK2 inhibitor

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

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

    AA26-9 is a potent and broad-spectrum serine hydrolase inhibitor.
  38. uPA inhibitor

    UK-371804 is a potent urokinase-type plasminogen activator (uPA) inhibitor.
  39. NAE inhibitor

    ZM223 is a non-sulfamide NEDD8 activating enzyme (NAE) inhibitor that inhibits HCT116 colon cancer cells with an IC50 value of 100 nM.
  40. HIV-1 maturation inhibitor

    GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor. CAS: 1392312-45-6 (free base) 2023808-13-9 (HCl) 2023798-97-0 (HCl hydrate) 2097784-79-5 (oxalate)
  41. TACE/MMP inhibitor

    TMI-1 is a novel orally active dual inhibitor of ADAM17 (TACE) and MMP.
  42. pan-caspase inhibitor

    MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1, caspase-3, and caspase-6, 7, 8, and 9.
  43. MMP inhibitor

    Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.
  44. Calpain inhibitor

    SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly.
  45. HCV NS5A inhibitor

    Velpatasvir, also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor.
  46. MMP inhibitor

    Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
  47. HCV NS5A inhibitor

    Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
  48. HCV NS3/4A inhibitor

    Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
  49. MMP inhibitor

    Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
  50. Elastase release inhibitor

    Acetylglucosamine or N-acetylglucosamine is potentially for the treatment of irritable bowel syndrome. N-Acetylglucosamine (GlcNAc) is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. GlcNAc has been reported to be an inhibitor of elastase release from human polymorphonuclear leukocytes (range 8?C17% inhibition), however this is much weaker than the inhibition seen with N-acetylgalactosamine (range 92?C100%).

Items 101-150 of 1366

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