trypsin-like

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

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.

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

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

PF-07321332 is a potent and orally active inhibitor of SARS-CoV 3C-like protease (3CLPRO) .

PI-1840(IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM for caspase-like proteasomes.

Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]

N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride (N-alpha-Tosyl-L-lysine_chloromethyl_ketone_hydrochloride) is an inhibitor of trypsin-like protease and exhibits an inhibitory effect on IFN-γ activities.

Thrombin (MW 37kDa) is an allosteric serine protease with trypsin-like activity.

Alkaline tryptase-IN-1 (compound H-13) is an insecticide that targets alkaline trypsin-like enzymes. It has lethal concentration (LC50) values of 8.72, 13.77, 14.17, 12.96, and 12.35 μg mL against Schizaphis graminum, Sitobion avenae, Brevicoryne brassicae, Aphis gossypii, Aphis spiraecola, and Myzus persicae, respectively.

Collagenase (Type C, animal free) is a compound devoid of animal-derived components, exhibiting low trypsin-like activity akin to Type IV collagenase.

Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).

Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

Boc-LRR-AMC TFA is a fluorescent protease substrate used to detect the trypsin-like activity of the 26S proteasome or 20S proteasome core.

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, exhibiting a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].

CRA-2059 is a highly specific and selective tryptase inhibitor with a Ki of 620 pM for recombinant human tryptase-β (rHTβ) [1][2].

APC-6860 is a trypsin-like serine protease inhibitor with ( k_i ) values of 0.21, 0.44, 1.5, 16.8, 20, and 30 μM for uPA, trypsin, tryptase, tPA, thrombin, and factor Xa, respectively. It exhibits a selectivity ratio for tPA versus uPA of 80 and has ( k_i ) values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be utilized for cancer research.

20S Proteasome activator 1 is a 20S proteasome activator with IC50 values of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites, and 1.8 μM for caspase sites. It prevents the accumulation of pathogenic alpha-synuclein (A53T) mutants through translation in the cellular system, thereby reducing the probability of disease occurrence. 20S Proteasome activator 1 can be used to study neurodegenerative diseases.

1. Fraxinellone significantly reduced weight loss and diarrhea in mice and alleviated the macroscopic and microscopic signs of the disease. 2. Fraxinellone exhibited a variety of insecticidal activities including feeding-deterrent activity, inhibition of growth, and larvicidal activity. 3. Fraxinellone has effect in the midgut metabolism of Mythimna separata (M. separata), via protease (especially the weak alkaline trypsin-like enzyme), carboxylesterase and glutathione S-transferase.

Urokinase peptidolytic,Urokinase-type plasminogen activator (uPA) is a trypsin-like serine protease that exists as an inactive zymogen (pro-uPA) and requires proteolytic cleavage for its activation. once activated, it serves as the central catalyst in a proteolytic cascade that converts plasminogen to plasmin, a process critically involved in physiological and pathological thrombolysis and extracellular matrix degradation.

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with K i s of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa , Thrombin and tPA, respectively [1] [2] .

23-O-β-D-Glucopyranosyl-20-isoveratramine, extracted from nettles, shows promise as an anti-allergic agent. Nettle extract contains a range of COX-1, COX-2, 5-lipoxygenase, and trypsin-like inhibitors, as well as H1 antagonists. These compounds collectively help mitigate symptoms of seasonal allergies, allergic rhinitis, and other inflammatory diseases, offering both treatment and preventive benefits [1].

Boc-Leu-Gly-Arg-AMC is a specific fluorogenic substrate designed for the enzymatic detection and quantification of complement component C3/C5 convertases, coagulation factor Xa, and soybean trypsin-like enzyme activity. Boc-Leu-Gly-Arg-AMC is also susceptible to hydrolysis by macropain, a high molecular weight thiol proteinase isolated from human erythrocytes, making it a versatile tool for enzymatic assays.