2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cathepsin

Cathepsin

Cathepsin

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Cathepsins are protease enzymes, categorized into multiple families. Cathepsins can be serine protease, cysteine protease, or aspartyl protease. There are about 15 classes of cathepsins in humans (Cathepsin A, B, C, D, E, F, G, H, K, L, O, S, V, W, and Z). Cathepsins are active in the low pH milieu of lysosomes and are versatile in their functions. Like other enzymes, they are vital for the normal physiological functions such as digestion, blood coagulation, bone resorption, ion channel activity, innate immunity, complement activation, apoptosis, vesicular trafficking, autophagy, angiogenesis, proliferation, and metastasis, among scores of others.

Numerous pathologies have been attributed to the dysregulated cathepsins, some of which include arthritis, periodontitis, pancreatitis, macular degeneration, muscular dystrophy, atherosclerosis, obesity, stroke, Alzheimer's disease, schizophrenia, tuberculosis, and Ebola.

Cathepsin Isoform Specific Products:

Cathepsin Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-D0843
    N-Ethylmaleimide
    		Inhibitor 99.89%
    N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.
    N-Ethylmaleimide
  • HY-18234A
    Leupeptin hemisulfate
    		Inhibitor 99.39%
    Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.
    Leupeptin hemisulfate
  • HY-B0496
    PMSF
    		Inhibitor 99.32%
    PMSF (Phenylmethylsulfonyl fluoride) is a nonspecific and irreversible serine proteases inhibitor. PMSF inhibits some thiol proteases, non-protease enzymes, and acetylcholinesterase. PMSF can be used to prepare protein extracts from tissue and cell lysates.
    PMSF
  • HY-148905
    p-Aminophenylmercuric acetate
    		Activator 99.07%
    p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). P-Aminophenylmercuric acetate participates in the activation and inhibition of MMP-8 by attacking protein sulfhydryl or inducing cysteine switching reaction. p-Aminophenylmercuric acetate promotes the shedding of betacellulin precursor (pro-BTC). p-Aminophenylmercuric acetate influences the binding of agonists and antagonists to the opiate receptor.
    p-Aminophenylmercuric acetate
  • HY-P1645
    Papain
    Papain is a cysteine protease of the peptidase C1 family, which is used in food, pharmaceutical, textile, and cosmetic industries.
    Papain
  • HY-P5898
    Z-Val-Val-Nle-diazomethylketone
    		Inhibitor
    Z-Val-Val-Nle-diazomethylketone is a cathepsin S (CATS) inhibitor. Z-Val-Val-Nle-diazomethylketone significantly inhibits the IFNg-induced upregulation of the MHCII molecules HLA-DR and Ii-p33/35 with an increase of Ii-p10 protein level. Z-Val-Val-Nle-diazomethylketone can be used for dermatological diseases like psoriasis, atopic dermatitis and actinic keratosis research.
    Z-Val-Val-Nle-diazomethylketone
  • HY-106058
    NCO-700
    		Inhibitor
    NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.
    NCO-700
  • HY-14360
    MK 1256
    		Inhibitor
    MK 1256 is a highly selective and orally active inhibitor of tissue protease K (Cat K) with an IC50 of 0.62 nM. MK 1256 shows extremely high selectivity towards other tissue proteases (all > 1100 times), with only a slightly lower selectivity for tissue protease F (Cat F) (110 times). MK 1256 exhibits strong anti-bone resorption activity in the osteoporosis model of rhesus monkeys with ovariectomy. MK 1256 can be used for research on osteoporosis.
    MK 1256
  • HY-100229
    Aloxistatin
    		Inhibitor 99.94%
    Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
    Aloxistatin
  • HY-15282
    E-64
    		Inhibitor 99.96%
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
    E-64
  • HY-100350
    CA-074 methyl ester
    		Inhibitor 99.34%
    CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
    CA-074 methyl ester
  • HY-100223
    Calpeptin
    		Inhibitor 99.17%
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
    Calpeptin
  • HY-103350
    CA-074
    		Inhibitor 99.94%
    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
    CA-074
  • HY-W010347
    L-Homocysteine
    		Activator 98.0%
    L-Homocysteine, an amino acid, is a homocysteine that has L configuration. Homocysteine is an essential intermediate in normal mammalian metabolism of methionine. L-Homocysteine induces upregulation of Cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia.
    L-Homocysteine
  • HY-15533
    LY 3000328
    		Inhibitor 99.50%
    LY 3000328 (Z-FL-COCHO) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
    LY 3000328
  • HY-16594
    Lactacystin
    		Inhibitor 98.20%
    Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on[2] [6] .
    Lactacystin
  • HY-128140
    Z-FY-CHO
    		Inhibitor
    Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.
    Z-FY-CHO
  • HY-10042
    Odanacatib
    		Inhibitor 99.80%
    Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
    Odanacatib
  • HY-W011063
    Gly-Phe-β-naphthylamide
    		99.92%
    Gly-Phe-β-naphthylamide is the substrate of Cathepsin C. Gly-Phe-β-naphthylamide can be used to study intralysosomal hydrolysis, lysosomal membrane permeability, and the function of cathepsin C.
    Gly-Phe-β-naphthylamide
  • HY-119293
    K777
    		Inhibitor 99.77%
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
    K777
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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