Cathepsin Inhibitor

Z-Phe-Ala-diazomethylketone binds directly to Aβ42 monomers and small oligomers. Z-Phe-Ala-diazomethylketone inhibits the formation of Aβ42 dodecamers and inhibits Aβ42 fibril formation in the solution. Z-Phe-Ala-diazomethylketone has the potential for neurodegenerative disorders research.

Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC₅₀ values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively.

CatD-IN-1 (Compound 5) is a Cathepsin D inhibitor with an IC₅₀ of 0.44 μM. CatD-IN-1 holds potential for research in the field of osteoarthritis .

GB111-NH2 hydrochloride is a cysteine cathepsin inhibitor, and can be used for cancer study.

4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases.

Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.

AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .

Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain.

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with K_i value of 3.1 μM, also possesses declining PLA₂ inhibitory potency, IC₅₀s of 11 μM and 3.5 μM for Atg4B and PLA₂, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition.

Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.

CTSE Human Pre-designed siRNA Set A contains three designed siRNAs for CTSE gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cysteine Protease inhibitor hydrochloride, an inhibitor of Cysteine Protease, binds to acetylcholinesterase (AChE). Cysteine Protease inhibitor hydrochloride is applicable to the research of Alzheimer's disease.

CTSC Human Pre-designed siRNA Set A contains three designed siRNAs for CTSC gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ctsd Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ctsd gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.

CTSB Human Pre-designed siRNA Set A contains three designed siRNAs for CTSB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ac-PLVE-FMK (Ac-Pro-Leu-Val-Glu(OMe)-CH2F), a tetrapeptidyl m-FMKs, is a Cats inhibitor. Ac-PLVE-FMK can be used for the research of cancer.

Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro.

JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (K_i = 38 nM) and mast cell chymase (K_i = 2.3 nM), exhibits noteworthy antiinflammatory activity.

AZD5248 is an orally active, selective dipeptidyl peptidase 1 (cathepsin C) inhibitor, with IC₅₀ values of 1 nM and 17 nM against human CatC, 44 nM against human DPP1, and 67 nM against rat DPP1. It exhibits low clearance and high bioavailability in animal models. AZD5248 forms an irreversible covalent bond with the catalytic Cys234 residue of CatC, exerts reversible inhibition via its nitrile moiety, blocks CatC-dependent amyloid formation, and reduces the activation levels of neutrophil serine proteases in bone marrow and blood. AZD5248 reacts with aortic elastin aldehydes to form stable 4-imidazolinones, induces ultrastructural changes in aortic tissue, and has an α-amino acid-based backbone. AZD5248 reduces the severity of acute pancreatitis in mouse models. AZD5248 can be used in research on chronic obstructive pulmonary disease, acute pancreatitis, neurodegenerative diseases, lysosomal storage disorders, acute lung injury, cystic fibrosis, and neutrophil-mediated inflammatory diseases.