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. |
-
Nat Commun, 2023, 14(1):4066
-
Acta Pharm Sin B, 2022, 12(6):2869-2886
-
Theranostics, 2022, 12(14):6395-6408
|
|
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 (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. |
-
Cell Death Dis, 2024, 15(2):109
-
CNS Neurosci Ther, 2024, 30(6):e14822
-
Pathogens, 2023, 13(1)18
|
|
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. |
-
Nat Commun, 2024, 15(1):6519
-
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00097-2
-
Microb Pathog, 2022, 166:105558
|
|
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 Immunol, 2021, 206(4):797-806
-
Aging (Albany NY), 2020, 12(17):16820-16836
-
Front Microbiol, 2020, 10:2936
|
|
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. |
-
Front Oncol, 2019, 0.87569444444
-
J Biol Chem, 2018, 293(34):13112-13124
-
Invest Ophthalmol Vis Sci, 2016, 57(14):6461-6473
|
|
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
|
|
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, used to reduce perioperative blood loss and transfusion.
|
-
Elife, 2021, 10e65962
-
Autophagy, 2017, 13(3):538-553
|
|
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. |
|
|
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. |
- Nat Commun, 2023, 14(1):4066
- Acta Pharm Sin B, 2022, 12(6):2869-2886
- Theranostics, 2022, 12(14):6395-6408
|
|
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 (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. |
- Cell Death Dis, 2024, 15(2):109
- CNS Neurosci Ther, 2024, 30(6):e14822
- Pathogens, 2023, 13(1)18
|
|
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. |
- Nat Commun, 2024, 15(1):6519
- Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00097-2
- Microb Pathog, 2022, 166:105558
|
|
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 Immunol, 2021, 206(4):797-806
- Aging (Albany NY), 2020, 12(17):16820-16836
- Front Microbiol, 2020, 10:2936
|
|
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. |
- Front Oncol, 2019, 0.87569444444
- J Biol Chem, 2018, 293(34):13112-13124
- Invest Ophthalmol Vis Sci, 2016, 57(14):6461-6473
|
|
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
|
|
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, used to reduce perioperative blood loss and transfusion.
|
- Elife, 2021, 10e65962
- Autophagy, 2017, 13(3):538-553
|
|
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. |
|
|
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. |
|
|