Serine Protease

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Serine Protease Products

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  • Serine Protease Inhibitors (14)
  • New Serine Protease Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
S1386 Nafamostat mesilate (FUT-175) 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.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1811 Amiloride (MK-870) 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).
Adv Sci (Weinh), 2021, 8(13):2100962
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
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.
Front Oncol, 2019, 0.87569444444
J Biol Chem, 2018, 293(34):13112-13124
Invest Ophthalmol Vis Sci, 2016, 57(14):6461-6473
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
Front Pharmacol, 2021, 12:769647
Gene, 2021, 812:146097
Eur J Pharmacol, 2021, 905:174198
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
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.
J Immunol, 2021, 206(4):797-806
Aging (Albany NY), 2020, 12(17):16820-16836
J Immunol, 2020, ji2000091
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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118
Sci Rep, 2019, 9(1):715
Exp Cell Res, 2019, 382(2):111486
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.
Elife, 2021, 10e65962
Autophagy, 2017, 13(3):538-553
S7378 AEBSF HCl AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.
Int J Mol Sci, 2021, 22(7)3683
NMR Biomed, 2021, e4664
Front Cell Dev Biol, 2020, 8:269
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.
Elife, 2021, 10e62394
Protein Cell, 2021, 10.1007/s13238-021-00858-3
Front Cell Dev Biol, 2021, 9:670145
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.
J Immunol, 2021, 206(4):797-806
J Cell Mol Med, 2021, 10.1111/jcmm.16555
Ecotoxicol Environ Saf, 2021, 211:111900
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).
Front Genet, 2021, 12:651882
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.
S1386 Nafamostat mesilate (FUT-175) 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.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1811 Amiloride (MK-870) 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).
Adv Sci (Weinh), 2021, 8(13):2100962
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
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.
Front Oncol, 2019, 0.87569444444
J Biol Chem, 2018, 293(34):13112-13124
Invest Ophthalmol Vis Sci, 2016, 57(14):6461-6473
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
Front Pharmacol, 2021, 12:769647
Gene, 2021, 812:146097
Eur J Pharmacol, 2021, 905:174198
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
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.
J Immunol, 2021, 206(4):797-806
Aging (Albany NY), 2020, 12(17):16820-16836
J Immunol, 2020, ji2000091
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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118
Sci Rep, 2019, 9(1):715
Exp Cell Res, 2019, 382(2):111486
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.
Elife, 2021, 10e65962
Autophagy, 2017, 13(3):538-553
S7378 AEBSF HCl AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.
Int J Mol Sci, 2021, 22(7)3683
NMR Biomed, 2021, e4664
Front Cell Dev Biol, 2020, 8:269
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.
Elife, 2021, 10e62394
Protein Cell, 2021, 10.1007/s13238-021-00858-3
Front Cell Dev Biol, 2021, 9:670145
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.
J Immunol, 2021, 206(4):797-806
J Cell Mol Med, 2021, 10.1111/jcmm.16555
Ecotoxicol Environ Saf, 2021, 211:111900
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).
Front Genet, 2021, 12:651882
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.
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.