trypsin-like

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

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]

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.

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

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

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.

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.

N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible serine protease inhibitor that functions by alkylating the histidine residue at the active site, thus inhibiting trypsin and trypsin-like proteases. It effectively inhibits caspase-3, caspase-6, and caspase-7 with IC50 values of 12.0, 54.5, and 19.3 μM, respectively. Additionally, N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in HL-60 cells and prevents the reduction of mitochondrial transmembrane potential during the apoptosis process.

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.

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).

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].