proteases

Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).

Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.

Proteinase K (Protease K) is a non-specific serine protease that can tolerate changes in SDS, urea, pH (4-12), salt concentration, and temperature. Proteinase K hydrolyzes a wide range of peptide bonds and is used for protein digestion.

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

Osemozotan Free Base is a 5-HT(1A) receptor agonist.

Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.

Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.

Nafamostat mesylate (FUT-175), a synthetic serine protease inhibitor, has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.

1-Dodecylimidazole (N-Dodecylimidazole) is a chemical compound that acts as a cytotoxic agent and lysosomotropic detergent, inducing cell death through acid-dependent lysosomal accumulation, disrupting the lysosomal membrane, and releasing cysteine proteases into the cytoplasm. It also exhibits hypocholesterolemic and broad-spectrum antifungal activities.

AEBSF hydrochloride (Pefabloc SC) is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, thrombin, plasmin, and trypsin.

Gastric mucin, a large glycoprotein, is thought to play a major role in protecting the gastrointestinal tract from acid, proteases, pathogenic microorganisms, and mechanical trauma. Gastric mucin is a natural protein derived from pigs.

Complement C1s-IN-1 is a potent and selective inhibitor of complement C1s with the advantage of being orally available and brain penetrable, significantly inhibiting human serum-induced formation of membrane attack complexes in a dose-dependent manner and effectively blocking the classical complement pathway

Cetraxate hydrochloride (DV10062) is an oral gastrointestinal medication. It has a cytoprotective effect.

BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).

Cysteine protease inhibitors are inhibitors of cysteine proteases. Target: Cysteine Protease

IPR-803 is an effective inhibitor of the uPAR·uPA protein-protein interaction (PPI) with anti-tumor activity. IPR-803 binds directly to uPAR with a Ki of 0.2 μM.

Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor that targets and inhibits the activity of gingipains, which are proteases involved in periodontal disease.

LSP-249 is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.

NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.

Statine is a protease inhibitor that is active against pepsin and other acid proteases.

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.