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-129578
    Asperphenamate
    		Inhibitor 98.0%
    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.
    Asperphenamate
  • HY-P1759A
    N-CBZ-Phe-Arg-AMC hydrochloride
    		Substrate 99.40%
    N-CBZ-Phe-Arg-AMC (Z-FR-AMC) hydrochloride is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes.
    N-CBZ-Phe-Arg-AMC hydrochloride
  • HY-100227
    E 64c
    		Inhibitor 99.32%
    E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
    E 64c
  • HY-148298
    CatD-IN-1
    		Inhibitor 99.27%
    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 .
    CatD-IN-1
  • HY-D1634
    Bz-FVR-AMC
    		99.83%
    Bz-FVR-AMC is a fluorogenic substrate for procathepsin with a kcat/Km value of 1070 mM-1s-1. The high concentration of BZ-FVR-AMC inhibits the substrate.
    Bz-FVR-AMC
  • HY-164278
    diABZI-V/C-Mal
    		Substrate 99.28%
    diABZI-V/C-Mal is a STING agonist (with a STING EC50 of 314 nM in TH1 dual reporter cells) and a Cathepsin B substrate. diABZI-V/C-Mal activates STING, thereby triggering the IRF3 signaling pathway. diABZI-V/C-Mal is cleaved by Cathepsin B to regenerate diABZI-NH2.
    diABZI-V/C-Mal
  • HY-N4288
    4-Methylesculetin
    		Inhibitor 99.27%
    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.
    4-Methylesculetin
  • HY-P1759
    N-CBZ-Phe-Arg-AMC
    		Substrate 99.88%
    N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes.
    N-CBZ-Phe-Arg-AMC
  • HY-N4289
    3-Epiursolic Acid
    		Inhibitor 99.77%
    3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
    3-Epiursolic Acid
  • HY-W790014
    Z-FG-NHO-BzOME
    		Inhibitor 98.02%
    Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain.
    Z-FG-NHO-BzOME
  • HY-112318A
    GSK-2793660
    		Inhibitor 99.91%
    GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.
    GSK-2793660
  • HY-W653733
    L-Homocysteine-d4
    L-Homocysteine-d4 is deuterium labeled L-Homocysteine (HY-W010347). 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-d<sub>4</sub>
  • HY-115454A
    GB111-NH2 hydrochloride
    		Inhibitor 98.93%
    GB111-NH2 hydrochloride is a cysteine cathepsin inhibitor, and can be used for cancer study.
    GB111-NH2 hydrochloride
  • HY-N6037
    Gardenin B
    		Inhibitor 99.69%
    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.
    Gardenin B
  • HY-P2922
    Cathepsin C
    Cathepsin C is a lysosomal cysteine protease essential for catalytic activation of many serine proteases, including proteinase 3 (PR3), neutrophil elastase (NE), cathepsin G (CTSG), granzyme A/B/C, and mast cell chymase.
    Cathepsin C
  • HY-P4340A
    Arg-Arg-AMC acetate
    		99.93%
    Arg-Arg-AMC acetate is the acetate salt form of Arg-Arg-AMC (HY-P4340). Arg-Arg-AMC acetate is a fluorescent substrate for cathepsin B and used in the cathepsin B activity assay.
    Arg-Arg-AMC acetate
  • HY-Y0241
    2-Cyanopyrimidine
    		Inhibitor 99.92%
    2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos.
    2-Cyanopyrimidine
  • HY-153986
    AEP-IN-2
    		Inhibitor 99.13%
    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 .
    AEP-IN-2
  • HY-108044
    ONO-5334
    		Inhibitor 99.83%
    ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
    ONO-5334
  • HY-P3012
    Cathepsin G
    Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases.
    Cathepsin G
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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