Cathepsin Inhibitor 1

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.

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.

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 is a bioactive dipeptide that can be used for the research of bronchiectasis [1] [2].

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].

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).

CZP-IN-1 (compound SH-1) is an inhibitor targeting the pathogen Trypanosoma cruzi protease (CZP) without affecting cathepsin L (IC50=28 nM). This compound is applicable in Chagas disease research.

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

Mpro/Cathepsin L-IN-1 (Compound 4d) is an inhibitor of SARS-CoV-2 Mpro and hCatL, with Ki values of 5.54 μM and 0.701 μM, respectively.

SmCB1-IN-1 (Compound 2h) is an inhibitor of the Schistosoma mansoni cathepsin B1 (SmCB1) with a Ki of 0.05 μM. It demonstrates selectivity towards non-target human proteases, showing inhibition rates of 29% for CatB and 37% for CatL at 20 μM. At 1 μM, SmCB1-IN-1 inhibits 68% of Schistosoma mansoni.

Mpro/Cathepsin L-IN-2 (Compound 1) is an irreversible dual inhibitor targeting the main protease of SARS-CoV-2 (Mpro, pIC50=8.61) and human cathepsin L (hCTSL, pIC50=7.64). Mpro/Cathepsin L-IN-2 shows potential for use in research related to COVID-19 and other coronavirus infections.

DPP-1-IN-1 (Compound 14) is an orally active inhibitor of cathepsin C (also known as dipeptidyl peptidase I), with an IC50 of 5.31 nM. It effectively suppresses downstream neutrophil elastase activity in neutrophils mediated by cathepsin C. DPP-1-IN-1 is applicable for studying inflammatory diseases.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.1It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50= 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50= 5.33 μM) but not cathepsin B when used at a concentration of 20 μM. 1.()

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

Odanacatib is an inhibitor of cathepsin K with potential anti-osteoporotic activity.

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].

Gü2602 inhibits the cathepsin K zymogen autocatalytic activation that is a potent, reversible inhibitor of cathepsin K (CatK) with a Ki of 0.013 nM for mature CatK (mCatK) [1].

Gü1303 is a highly potent and reversible inhibitor of Cathepsin K (CatK), with a Ki value of 0.91 nM for mature CatK (mCatK). This compound effectively suppresses the autocatalytic activation of the CatK zymogen [1].

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].

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 C-IN-3 is a potent inhibitor of histone C (IC50: 61.79 nM) and also inhibits THP-1 cells (IC50: 101.5 nM) and U937 cells (IC50: 86.5 nM).

Calpeptin is a cell-permeable Calpain inhibitor (IC50 = 5 nM), and its ID50 value for human platelet Calpain I is 40 nM. Calpeptin is also an effective inhibitor of Cathepsin K (IC50 = 0.11 nM).

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.