Chymotrypsin A

TLCK-treated Chymotrypsin is a type of serine protease that cleaves protein chains at the carboxyl side of aromatic amino acids. It undergoes TLCK treatment to inactivate residual trypsin activity.

Chymotrypsin-IN-1 (Compound TPCK) is an inhibitor of chymotrypsin, capable of irreversibly inhibiting chymotrypsin-like serine proteases.

Chymotrypsin (Chymotrypsin A) is a serine protease synthesized by the pancreas, which cleaves protein chains on the carboxyl side of aromatic amino acids.

Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

Carfilzomib (PR-171) is a proteasome inhibitor that irreversibly binds to the chymotrypsin of the 20S proteasome. Carfilzomib has antitumor activity and may be used to treat multiple myeloma.

L-Serine (serine) is a non-essential amino acid in humans, L-Serine is present and functionally important in many proteins.L-Serine is also found at the active site of the serine protease enzyme class that includes trypsin and chymotrypsin.

GSK3494245 is a Leishmania donovani inhibitor that suppresses trypsin-like activity catalyzed by the β5 subunit of L. donovani proteasome, applicable for visceral leishmaniasis (VL) studies.

CDD-3290 represents a highly specialized small molecule inhibitor specifically engineered to target the catalytic activity of Prostate-Specific Antigen (PSA/KLK3) with exceptional inhibitory potency. It effectively facilitates the measurable blockade of PSA-mediated proteolytic cleavage across various preclinical experimental models to evaluate the disruption of the tumor microenvironment during strictly monitored laboratory observation periods and enzyme kinetic assays to ensure high experimental sensitivity.

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.

Aclacinomycin A hydrochloride (Aclarubicin HCl) is an anthracycline antibiotic and inhibitor of topoisomerase I/II, interfering with DNA transcription and replication, inhibiting tumour invasion and angiogenesis, generating reactive oxygen species (ROS), and inhibiting the catalytic centre of the 20S proteasome. It is indicated for the treatment of relapsed leukaemia and advanced malignant lymphoma.

FK-448 Free base is a potent and specific chymotrypsin inhibitor, with an IC50 of 720 nM.

The bentiromide test is an excellent means of confirming the diagnosis of pancreatic exocrine insufficiency by outpatient test of chymotrypsin function[1]. Bentiromide is a peptide which is broken down in the pancreas by chymotrypsin.

Bentiromide acetate is a peptide used as a screening test for exocrine pancreatic insufficiency and to monitor the adequacy of supplemental pancreatic therapy. It is broken down by the pancreatic enzyme chymotrypsin, yielding p-aminobenzoic acid (PABA).

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

Caspase-3-IN-2 (Compound 4d) acts as an inhibitor of α-Chymotrypsin. It also exhibits inhibitory activity against HIV protease and caspase 3, with inhibition rates of 57% and 51% respectively at a concentration of 100 μM.

PROTACKRAS G12D degrader 2 is a peptidomimetic molecule capable of inducing the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro). Designed as a PROTAC molecule, it combines a dipeptidyl 3CLPro ligand based on GC-376 with a pomalidomide moiety, linked through a piperazine-piperidine linker.

20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S proteasome, with IC50 values of 0.19 μM for chymotrypsin-like (ChT-L) activity and 52.5 μM for peptidylglutamyl-peptide hydrolyzing-like (PGPH-L) activity.

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).

L 373890 is a selective pyridoneacetamide inhibitor of thrombin (thrombin) with a Ki value of 0.5 nM. It demonstrates significantly higher selectivity for thrombin compared to trypsin (Ki value of 570 nM), as well as serine proteases, plasmin, tPA, activated protein C, plasma kallikrein, and chymotrypsin. L 373890 is utilized in thrombosis research.

INVA8001 is a highly selective and orally active chymase inhibitor, with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell protease 4 (mMCP-4). It exhibits IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, demonstrating over 1000-fold selectivity against other related serine proteases. In a mouse model of primary sclerosing cholangitis (PSC), INVA8001 inhibits mast cell activity, improves biliary pathology, alleviates cholestasis, and displays anti-inflammatory and anti-fibrotic properties.

AMC-3-030 is a selective and potent dual inhibitor targeting HDAC6 and chymotrypsin-like proteasome, with IC50 values of 884 nM and 4.17 nM, respectively. It inhibits cell proliferation and reduces levels of α-tubulin and β-actin. AMC-3-030 is applicable in the research of multiple myeloma.

MG-115 (Z-LL-Nva-CHO) is a potent and reversible inhibitor of proteasome , with K i s of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis [1] [2] [3].

RETF-4NA acetate is a sensitive, specific substrate for chymotrypsin.

Cyanopeptolin 954 is a chlorine-containing Microcystis aeruginosa NIVA Cya 43 chymotrypsin Inhibitor.