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Proteases

Proteases, also known as peptidases or proteolytic enzymes, consists of a large number of enzymes catalyzing the hydrolysis of peptide bonds and subsequently resulting in the degradation of protein substrates into amino acids. Proteases are involved in a wide range of human diseases, including cancer, neurodegenerative disorders, inflammatory diseases and cardiovascular diseases. Thus numerous proteases inhibitors (small molecules and proteins) have been identified to block activity of proteases. Proteases inhibitors can be classified into different types based on the class of proteases they inhibit through two general mechanisms, irreversible “trapping” reactions and reversible tight-binding reactions. Proteases inhibitors have been used as diagnostic or therapeutic agents for the treatment of proteases-related diseases.

Products for  Proteases

  1. Cat.No. Product Name Information
  2. A4022 BMS-708163 (Avagacestat) BMS-708163 is a potent selective and orally bioavailable inhibitor of γ-secretase with IC50 value of 0.3nM .
  3. A8200 DAPT (GSI-IX) DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.
  4. A8189 PSI-6206 PSI-6206 (as known as RO-2433 or GS-331007), β-D-2’-deoxy-2’-fluoro-2’-C-methyluridine, is the deaminated derivative of PSI-6130, β-D-2’-deoxy-2’-fluoro-2’-C-methylcytidine, which is a potent inhibitor of hepatitis C virus (HCV) replication in the subgenomic HCV reolicon system.
  5. A8170 Z-FA-FMK An inhibitor of cysteine proteases, such as cathepsin B, which do not require a P1 Asp residue.
  6. A1901 Q-VD-OPh hydrate

    Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).

  7. A2588 PPACK Dihydrochloride PPACK Dihydrochloride is the dihydrochloride form of its active component PPACK (D-Phenylalanyl-L-prolyl-L-arginine chloromethyl ketone), a potent, selective and irreversible inhibitor of thrombin that inhibits human α-thrombin with inhibition constant Kivalue of 0.24 nM.
  8. A2585 MG-132

    MG132 (carbobenzoxy-Leu-Leu-leucinal) as a peptide aldehyde effectively blocks the proteolytic activity of proteasome complex.

  9. A8204 Lopinavir Lopinavir (also known as ABT-378) is a highly potent inhibitor of human immunodeficiency virus (HIV) protease that potently inhibits wild-type and mutant HIV protease with inhibition constant Ki values ranging from 1.3 to 3.6 pM.
  10. A2577 Batimastat (BB-94)

    Batimastat (also known as BB-49), [4-(N-hydroxyamino)-2R-isobutyl-3S-(thiopen-2-ylthiomethyl)-succinyl-L-phenylalanine-N-methylamide, 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).

  11. A2575 Bestatin Ubenimex(Bestatin) is a specific inhibitor of aminopeptidase B and leucine aminopeptidase. It did not show any inhibition of aminopeptidase A, trypsin, chymotrypsin, elastase..

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