Inhibitors


The main physiological inhibitors of the coagulation proteases are members of the serpin family, e.g. antithrombin (AT, previously known as antithrombin III or ATIII), heparin cofactor II (HCII), protease nexin 1 (PN1), alpha-1-antitrypsin (α1AT) and protein C inhibitor (PCI). With the exeption of α1AT, all are activated by glycosaminoglycans, such as heparin. The serpin mechanism of inhibition is well characterised, with formation of an initial recognition complex followed by a rapid serpin conformational change that traps and deforms the protease as a covalent acyl-enzyme intermediate.

Alpha-2-Macroglobulin (a2M) is a general inhibitor that has the ability to inhibit proteases from all classes. The mechanism involves protease cleavage of a bait region initiating a large conformational change that effectively traps the protease in a molecular cage.

Alpha-1-antitrypsin

  • Human alpha-1 antitrypsin (plasma)

     
    Human alpha-1 antitrypsin (plasma).
    Species: Human Source: Natural Expression: N/A Cell Line: N/A Sequence Type: Wild-type
  • Human alpha-1 antitrypsin (C232S)

     
    Human alpha-1 antitrypsin (C232S) recombinant mammalian expression. The C232S mutation prevents oxidation of this residue, including disulphide bond formation.
    Species: Human Source: Recombinant Expression: Mammalian Cell Line: HEK EBNA Sequence Type: Wild-type
  • Human alpha-1 antitrypsin (C232S)

     
    Human alpha-1 antitrypsin (C232S) recombinant bacterial expression. This protein has an N-terminal His tag. The C232S mutation prevents oxidation of this residue, including disulphide bond formation.
    Species: Human Source: Recombinant Expression: Bacterial Cell Line: E coli Sequence Type: Wild-type
  • Human alpha-1 antitrypsin Pittsburgh (M358R/C232S)

     
    Human alpha-1 antitrypsin Pittsburgh (M358R/C232S) recombinant bacterial expression. This protein has an N-terminal His tag. The Pittsburgh mutation turns antitrypsin into a potent inhibitor or thrombin. The C232S mutation prevents oxidation of this residue, including disulphide bond formation.
    Species: Human Source: Recombinant Expression: Bacterial Cell Line: E coli Sequence Type: Mutant
  • Human alpha-1 antitrypsin Pittsburgh (M358R/C232S)

     
    Human alpha-1 antitrypsin Pittsburgh (M358R/C232S) recombinant mammalian expression. The Pittsburgh mutation turns antitrypsin into a potent inhibitor or thrombin. The C232S mutation prevents oxidation of this residue, including disulphide bond formation. (Publications)
    Species: Human Source: Recombinant Expression: Mammalian Cell Line: HEK EBNA Sequence Type: Mutant

Alpha-2-macroglobulin

  • Human alpha-2-macroglobulin (plasma) open/active form

     
    Human alpha-2-macroglobulin (plasma) open/active form
    Species: Human Source: Recombinant Expression: N/A Cell Line: N/A Sequence Type: Wild-type

Antithrombin

  • Human alpha-antithrombin (plasma)

     
    Human alpha-antithrombin (plasma)
    Species: Human Source: Natural Expression: N/A Cell Line: N/A Sequence Type: Wild-type
  • Human beta-antithrombin (S137A)

     
    Human beta-antithrombin (S137A) recombinant mammalian expression.
    Species: Human Source: Recombinant Expression: Mammalian Cell Line: HEK EBNA Sequence Type: Mutant

Protein C inhibitor

  • Human Protein C Inhibitor (wild-type)

     
    Human Protein C Inhibitor (wild-type) recombinant bacterial expression.
    Species: Human Source: Recombinant Expression: Bacterial Cell Line: E coli Sequence Type: Wild-type
  • Human Protein C Inhibitor (delta21)

     
    Human Protein C Inhibitor (delta 21) recombinant bacterial expression. This lacks the first 21 N-terminal amino acids.
    Species: Human Source: Recombinant Expression: Bacterial Cell Line: E coli Sequence Type: Mutant

Protease nexin 1

  • Human protease nexin 1 (wild-type)

     
    Human protease nexin 1 (wild-type) recombinant bacterial expression.
    Species: Human Source: Recombinant Expression: Bacterial Cell Line: E coli Sequence Type: Wild-type

Heparin cofactor II

  • Human heparin cofactor II (plasma)

     
    Human heparin cofactor II (plasma).
    Species: Human Source: Natural Expression: N/A Cell Line: N/A Sequence Type: Wild-type