Serine Protease

Inhibitory Selectivity

Serine Protease Products

Catalog No. Information Product Use Citations Product Validations
S1386

Nafamostat Mesylate

Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.

S1811

Amiloride HCl

Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

S3025

PMSF

PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.

S2101

Gabexate Mesylate

Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.

S0042

Fulacimstat

Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.

S0479New

ZK824859

ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.

S7218

Alvelestat (AZD9668)

Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.

S7378

AEBSF HCl

AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.

S7380

Leupeptin Hemisulfate

Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.

S8457

UK-371804 HCl

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

S4666

Sivelestat sodium tetrahydrate

Sivelestat sodium tetrahydrate (ONO5046-Na, EI546, LY544349) is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

S8136

Sivelestat (ONO-5046)

Sivelestat (ONO5046, LY544349, EI546) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.

S7377

Aprotinin

Aprotinin is a small protein serine protease inhibitor (Kd=0.06 pM for bovine β-trypsin), used to reduce perioperative blood loss and transfusion.

Catalog No. Information Product Use Citations Product Validations
S1386

Nafamostat Mesylate

Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.

S1811

Amiloride HCl

Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

S3025

PMSF

PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.

S2101

Gabexate Mesylate

Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.

S0042

Fulacimstat

Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.

S0479New

ZK824859

ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.

S7218

Alvelestat (AZD9668)

Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.

S7378

AEBSF HCl

AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.

S7380

Leupeptin Hemisulfate

Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.

S8457

UK-371804 HCl

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

S4666

Sivelestat sodium tetrahydrate

Sivelestat sodium tetrahydrate (ONO5046-Na, EI546, LY544349) is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

S8136

Sivelestat (ONO-5046)

Sivelestat (ONO5046, LY544349, EI546) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.

S7377

Aprotinin

Aprotinin is a small protein serine protease inhibitor (Kd=0.06 pM for bovine β-trypsin), used to reduce perioperative blood loss and transfusion.