Proteases

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. HIV Protease Inhibitor

    Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
  2. 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).
  3. 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.
  4. aldose reductase inhibitor

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

    Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.
  7. 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.
  8. 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.
  9. HIV protease inhibitor

    Darunavir Ethanolate (Prezista) is an HIV protease inhibitor.
  10. Indinavir sulfate is a novel hydroxyaminopentane amide class of HIV-1 protease inhibitors.
  11. Serine/cysteine protease inhibitor

    PMSF is an irreversible serine/cysteine protease inhibitor.
  12. 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
  13. Amprenavir is an human immunodeficiency virus (HIV) protease inhibitor with IC50 of 14.6 ?? 12.5 ng/ml for wild-type HIV isolates
  14. 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)
  15. Cathepsin K inhibitor

    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys.
  16. p32-kinase activator

    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  17. Pan Caspase Inhibitor

    Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.
  18. gamma-secretase modulator

    Flurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.
  19. Thrombin inhibitor

    Ximelagatran is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy.
  20. DPP-IV Inhibitor

    Vildagliptin is a dipeptidyl peptidase-4 (CD26) inhibitor.
  21. Caspase-6 inhibitor

    Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability.
  22. Caspase-2 inhibitor

    Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes.
  23. Immunoproteasome inhibitor

    ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome.
  24. Caspase-3 inhibitor

    Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.
  25. MTP inhibitor

    Lomitapide is a potent microsomal triglyceride transfer protein (MTP) inhibitor.
  26. neutrophil elastase inhibitor

    Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE).
  27. PPP1R15A inhibitor

    Sephin1 is a selective inhibitor of stress-induced PPP1R15A and targets disease associated with accumulation of misfolded protein.
  28. SHIP1 Inhibitor

    3AC is a cell-permeable, selective inhibitor of SHIP1 polyphosphatase activity toward PIP3 (IC50 = 10 μM), but has no effect on SHIP2 or PTEN activity on PIP3.
  29. MMP inhibitor

    Marimastat acted as a broad-spectrum matrix metalloproteinase inhibitor.
  30. HIV-1 Vif inhibitor

    RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC50 of 6 μM in nonpermissive H9 cells.
  31. MMP inhibitor

    Batimastat (BB-94) is a potent and synthetic inhibitor of a broad spectrum of matrix metalloproteinases (MMPs), including interstitial collagenase (IC50 = 3 nM), stromelysin (IC50 = 20 nM), Mr 72,000 type IV collagenase (IC50 = 4 nM), Mr 92,000 type IV collagenase (IC50 = 4 nM), and matrilysin (IC50 = 6 nM). It is a low-molecular-weight (MW = 478) and peptide-like collagen substrate analogue consisting of a peptide backbone and a hydroxamic acid group which bind to MMPs and the catalytically active zinc atom respectively.
  32. Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
  33. Apoptosis inducer

    LY573636 is a potent anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636-induced apoptosis occurs by a mitochondrial-targeted mechanism.
  34. MT1-MMP inhibitor

    NSC-405020 is a membrane type-1 matrix metalloproteinase (MT1-MMP) inhibitor (IC50 > 100 μmol/L).
  35. NS5A inhibitor

    Ledipasvir is an inhibitor of the hepatitis C virus HCV NS5A protein
  36. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
  37. HIV-1 RT inhibitor

    Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate.
  38. Cathepsin B inhibitor

    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
  39. Cysteine Protease inhibitor

    E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain.
  40. Cysteine Protease inhibitor

    Loxistatin Acid, a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
  41. Cysteine Protease inhibitor

    E-64d is an inhibitor of cathepsins B and L and it is lysosome and cell permeable.
  42. DPP-4 inhibitor

    Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
  43. DPP-4 inhibitor

    Alogliptin Benzoate is a dipeptidyl-peptidase-4 (DPP 4) inhibitor
  44. DPP-4 inhibitor

    Trelagliptin is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).
  45. dual TACE/MMPs inhibitor

    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) .
  46. 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).
  47. 4-Butylresorcinol is a phenol derivative which can inhibit tyrosinase with IC50 of 11.27 μM.
  48. Caspase-3 Inhibitor

    Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.
  49. 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.
  50. 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.

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