| S7380 |
Leupeptin Hemisulfate
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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.
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Adv Mater, 2025, e18445.
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Nat Commun, 2025, 16(1):4069
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J Adv Res, 2025, S2090-1232(25)00056-6
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| S3025 |
PMSF
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PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
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Cell Death Discov, 2024, 10(1):171
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Cell Biosci, 2023, 13(1):9
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Cell Mol Immunol, 2022, 19(10):1153-1167
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| S1386 |
Nafamostat mesilate (FUT-175)
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Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor used as an anticoagulant during hemodialysis. It blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. This compound also attenuates inflammation and apoptosis.
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J Immunother Cancer, 2024, 12(11)e009805
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Cell Death Dis, 2024, 15(2):109
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CNS Neurosci Ther, 2024, 30(6):e14822
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| S8136 |
Sivelestat
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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.
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Redox Biol, 2025, 87:103881
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J Immunother Cancer, 2025, 13(2)e010813
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Int Immunopharmacol, 2025, 151:114340
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| S7378 |
AEBSF HCl
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AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.
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Acta Pharm Sin B, 2025, 15(10):5277-5293
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Acta Pharm Sin B, 2024, 14(6):2554-2566
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Int J Med Sci, 2024, 21(7):1204-1212
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| S2101 |
Gabexate Mesylate
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Gabexate Mesylate (FOY) is a serine protease inhibitor with an IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.
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Trends Biotechnol, 2025, S0167-7799(25)00406-8
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iScience, 2024, 27(10):110862
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Curr Res Chem Biol, 2022, 2:100023
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| S7218 |
Alvelestat (AZD9668)
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Alvelestat (AZD9668) 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 Protease. This compound is in Phase 2.
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Cell Death Discov, 2025, 11(1):29
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Int Immunopharmacol, 2025, 159:114860
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Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118
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| S4666 |
Sivelestat sodium tetrahydrate
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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.
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J Thorac Dis, 2024, 16(10):6616-6633
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J Immunol, 2021, 206(4):797-806
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Aging (Albany NY), 2020, 12(17):16820-16836
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| S7377 |
Aprotinin
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Aprotinin is a small protein serine protease inhibitor (Kd=0.06 pM for bovine β-trypsin), used to reduce perioperative blood loss and transfusion.
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Front Cell Neurosci, 2025, 19:1623747
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J Immunother Cancer, 2024, 12(11)e009805
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Elife, 2021, 10e65962
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| S8457 |
UK-371804 HCl
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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).
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PNAS Nexus, 2022, 1(3):pgac104
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Front Genet, 2021, 12:651882
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