cathepsin

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Papain, a cysteine protease of the peptidase C1 family, is utilized in the food, pharmaceutical, textile, and cosmetic industries.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

Balicatib (AAE581) is a potent and selective inhibitor of cathepsin K, used in trials studying the treatment of osteoporosis.

LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.

Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor (IC50 = 7.13 μM) that reduces PC-3 cell migration with low cytotoxicity [1].

Cathepsin K Inhibitor7 (compound 7) is an inhibitor of Cathepsin K, exhibiting a pKi value of 7.3. It is utilized in research on osteoporosis.

CathepsinL-IN-5 (D6-3) is a potent inhibitor of Cathepsin L (CatL) with an IC50 value of 0.27 nM. It effectively blocks the function of CatL and significantly impedes the entry of SARS-CoV-2 pseudovirus into cells by inhibiting the cleavage of the spike protein. CathepsinL-IN-5 is applicable for research on infections.

Cathepsin L-IN-3, a tripeptide-sized inhibitor of cathepsin L, effectively targets this specific enzyme.

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

Cathepsin C-IN-6 (compound 2), an E-64c-hydrazideas-derived inhibitor of cathepsin C, possesses anti-inflammatory properties and impedes neutrophil elastase activation, demonstrating potential efficacy in treating inflammatory diseases characterized by elevated neutrophil counts, such as chronic obstructive pulmonary disease (COPD) [1].

Cathepsin L S-IN-1, a dual inhibitor targeting Cathepsin L and Cathepsin S, exhibits potent and selective inhibition with IC50 values of 4.10 μM and 1.79 μM, respectively. Demonstrating significant antimetastatic and invasive effects, it effectively impacts pancreatic cancer BxPC-3 and PANC-1 cells.

DualCathepsinL JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1 2 3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL JAK-IN-1 is applicable in research on acute lung injury (ALI).

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate selectively cleaved by cathepsins D and E at the Phe-Phe amide bond, demonstrating no activity towards cathepsins B, H, or L. This specificity renders it essential for routine assays and mechanistic studies focusing on cathepsins E and D[1].

Mca-GKPILFFRL-Dpa-r-amide, FRET substrate for cathepsin D and E. Also cleaved by napsin A.

Cathepsin B is a cysteine protease located within the subcellular endosomes and lysosomal compartments that mediates apoptosis and can be used in cancer research.

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K, a cysteine protease expressed under the control of the CTSK gene, which is closely related to osteoporosis and hydrolyses collagen. Cathepsin K inhibitor 2 has shown potential in osteoarthritis.

Cathepsin G is a potent agonist of human platelet activation, leading to aggregation, and can be used for screening relevant inhibitors [1].

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).

Cathepsin C-IN-4 is a potent inhibitor (IC50: 65.6 nM) of histone C. Cathepsin C-IN-4 inhibits THP-1 cells (IC50: 203.4 nM) and U937 cells (IC50: 177.6 nM).

Cathepsin G(1-5), an antimicrobial peptide identified within the clostripain-digested cathepsin G mixture [1], exhibits bactericidal properties.

Cathepsin C-IN-5 (compound SF38) is a potent, selective, and orally active Cathepsin C inhibitor with an IC50 of 59.9 nM for Cat C, and significantly lower potency against Cat L (4.26 µM), Cat S, Cat B, and Cat K (all >5 µM). It reduces Cat C activity in bone marrow and blood, diminishes NSPs activation, and exhibits anti-inflammatory activity [1].