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-103352
    L-006235
    		Inhibitor 99.96%
    L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.
    L-006235
  • HY-114374
    RO5461111
    		Antagonist 98.17%
    RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis.
    RO5461111
  • 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-P1315
    Papain inhibitor
    		Inhibitor 99.60%
    Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2.
    Papain inhibitor
  • HY-149482
    LN5P45
    		Inhibitor 99.05%
    LN5P45 is an OTUB2 inhibitor (IC50: 2.3 μM). LN5P45 induces monoubiquitination of OTUB2 on lysine 31. LN5P45 can be used for research of tumor progression and metastasis.
    LN5P45
  • HY-N2905
    Aurantiamide acetate
    		Inhibitor 99.85%
    Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases.
    Aurantiamide acetate
  • HY-141867
    Z-FF-FMK
    		Inhibitor 98.71%
    Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation.
    Z-FF-FMK
  • HY-P4515
    Z-Phe-Arg-pNA
    		99.95%
    Z-Phe-Arg-pNA is a substrate of Cathepsin L.
    Z-Phe-Arg-pNA
  • HY-115454A
    GB111-NH2 hydrochloride
    		Inhibitor 99.26%
    GB111-NH2 hydrochloride is a cysteine cathepsin inhibitor, and can be used for cancer study.
    GB111-NH2 hydrochloride
  • HY-P4295
    Z-Phe-Ala-diazomethylketone
    		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.
    Z-Phe-Ala-diazomethylketone
  • HY-N4288
    4-Methylesculetin
    		Inhibitor 98.21%
    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-155667A
    Z-Nle-Lys-Arg-AMC acetate
    		98.92%
    Z-Nle-Lys-Arg-AMC acetate is a fluorogenic peptide substrate that specifically monitors cathepsin B activity over a broad pH range.
    Z-Nle-Lys-Arg-AMC acetate
  • 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-P2498A
    Cathepsin D and E FRET Substrate acetate
    		99.78%
    Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.
    Cathepsin D and E FRET Substrate acetate
  • 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-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-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-15958
    VBY-825
    		Inhibitor 99.81%
    VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects.
    VBY-825
  • 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-W790014
    Z-FG-NHO-BzOME
    		Inhibitor 98.14%
    Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain.
    Z-FG-NHO-BzOME
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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