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. |
-
J Adv Res, 2025, S2090-1232(25)00056-6
-
J Transl Med, 2025, 23(1):62
-
iScience, 2025, 28(2):111804
|
|
S3025 |
PMSF
|
PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. |
-
Cell Death Discov, 2024, 10(1):171
-
Cell Biosci, 2023, 13(1):9
-
Cell Biosci, 2023, 13(1):9
|
|
S1811 |
Amiloride HCl
|
Amiloride HCl 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). |
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
-
Virus Res, 2024, 339:199258
|
|
S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate 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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cell Death Dis, 2024, 15(2):109
-
CNS Neurosci Ther, 2024, 30(6):e14822
|
|
S8136 |
Sivelestat
|
Sivelestat 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 Immunother Cancer, 2025, 13(2)e010813
-
Int Immunopharmacol, 2025, 151:114340
-
Nat Commun, 2024, 15(1):6519
|
|
S7378 |
AEBSF HCl
|
AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.
|
-
Acta Pharm Sin B, 2024, 14(6):2554-2566
-
Int J Med Sci, 2024, 21(7):1204-1212
-
Int J Biol Sci, 2023, 19(13):4327-4339
|
|
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 Thorac Dis, 2024, 16(10):6616-6633
-
J Immunol, 2021, 206(4):797-806
-
Aging (Albany NY), 2020, 12(17):16820-16836
|
|
S2101 |
Gabexate Mesylate
|
Gabexate Mesylate(FOY) is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation. |
-
Curr Res Chem Biol, 2022, 2:100023
-
Front Oncol, 2019, 0.87569444444
-
J Biol Chem, 2018, 293(34):13112-13124
|
|
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.
|
-
Cell Death Discov, 2025, 11(1):29
-
Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118
-
Sci Rep, 2019, 9(1):715
|
|
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). |
-
PNAS Nexus, 2022, 1(3):pgac104
-
Front Genet, 2021, 12:651882
|
|
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.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Elife, 2021, 10e65962
-
Autophagy, 2017, 13(3):538-553
|
|
E7249New |
Ulinastatin
|
Ulinastatin (Uristatin) is the main inhibitor of a hydrolase protein and serine protease suppresses trypsin, chymotrypsin, and other pancreatic proteases. It can inhibit the production and release of inflammatory factors through mediating inflammatory pathways, while modulating apoptosis, enzyme activity, coagulation, and immune responses. It is effective in preventing and managing conditions like pancreatitis, cerebral edema, acute respiratory distress, circulatory failure, sepsis, and systemic inflammatory response syndrome. |
|
|
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. |
|
|
S3511 |
FOY251
|
FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection. |
|
|
E1342 |
Sebetralstat
|
Sebetralstat(KVD900) is a plasma kallikrien inhibitor. |
|
|
E6013New |
Sivelestat sodium
|
Sivelestat sodium (ONO-5046, Sodium sivelestat, LY544349 sodium) is a potent, specific, and intravenously active inhibitor of neutrophil elastase with an IC50 value of 44 nm. It is a useful agent for studying the roles of neutrophil elastase in animal disease models such as emphysema, adult respiratory distress syndrome, septic shock and disseminated intravascular coagulation in COVID-19. |
|
|
E1014 |
Upamostat (WX-671)
|
Upamostat (WX-671), a novel serine protease urokinase (uPA) inhibitor by inhibiting the urokinase-type plasminogen activator (uPA) system. |
|
|
S0479 |
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. |
|
|
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. |
- J Adv Res, 2025, S2090-1232(25)00056-6
- J Transl Med, 2025, 23(1):62
- iScience, 2025, 28(2):111804
|
|
S3025 |
PMSF
|
PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. |
- Cell Death Discov, 2024, 10(1):171
- Cell Biosci, 2023, 13(1):9
- Cell Biosci, 2023, 13(1):9
|
|
S1811 |
Amiloride HCl
|
Amiloride HCl 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). |
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
- Virus Res, 2024, 339:199258
|
|
S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate 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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cell Death Dis, 2024, 15(2):109
- CNS Neurosci Ther, 2024, 30(6):e14822
|
|
S8136 |
Sivelestat
|
Sivelestat 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 Immunother Cancer, 2025, 13(2)e010813
- Int Immunopharmacol, 2025, 151:114340
- Nat Commun, 2024, 15(1):6519
|
|
S7378 |
AEBSF HCl
|
AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.
|
- Acta Pharm Sin B, 2024, 14(6):2554-2566
- Int J Med Sci, 2024, 21(7):1204-1212
- Int J Biol Sci, 2023, 19(13):4327-4339
|
|
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 Thorac Dis, 2024, 16(10):6616-6633
- J Immunol, 2021, 206(4):797-806
- Aging (Albany NY), 2020, 12(17):16820-16836
|
|
S2101 |
Gabexate Mesylate
|
Gabexate Mesylate(FOY) is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation. |
- Curr Res Chem Biol, 2022, 2:100023
- Front Oncol, 2019, 0.87569444444
- J Biol Chem, 2018, 293(34):13112-13124
|
|
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.
|
- Cell Death Discov, 2025, 11(1):29
- Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118
- Sci Rep, 2019, 9(1):715
|
|
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). |
- PNAS Nexus, 2022, 1(3):pgac104
- Front Genet, 2021, 12:651882
|
|
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.
|
- J Immunother Cancer, 2024, 12(11)e009805
- Elife, 2021, 10e65962
- Autophagy, 2017, 13(3):538-553
|
|
E7249New |
Ulinastatin
|
Ulinastatin (Uristatin) is the main inhibitor of a hydrolase protein and serine protease suppresses trypsin, chymotrypsin, and other pancreatic proteases. It can inhibit the production and release of inflammatory factors through mediating inflammatory pathways, while modulating apoptosis, enzyme activity, coagulation, and immune responses. It is effective in preventing and managing conditions like pancreatitis, cerebral edema, acute respiratory distress, circulatory failure, sepsis, and systemic inflammatory response syndrome. |
|
|
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. |
|
|
S3511 |
FOY251
|
FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection. |
|
|
E1342 |
Sebetralstat
|
Sebetralstat(KVD900) is a plasma kallikrien inhibitor. |
|
|
E6013New |
Sivelestat sodium
|
Sivelestat sodium (ONO-5046, Sodium sivelestat, LY544349 sodium) is a potent, specific, and intravenously active inhibitor of neutrophil elastase with an IC50 value of 44 nm. It is a useful agent for studying the roles of neutrophil elastase in animal disease models such as emphysema, adult respiratory distress syndrome, septic shock and disseminated intravascular coagulation in COVID-19. |
|
|
E1014 |
Upamostat (WX-671)
|
Upamostat (WX-671), a novel serine protease urokinase (uPA) inhibitor by inhibiting the urokinase-type plasminogen activator (uPA) system. |
|
|
S0479 |
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. |
|
|