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-134434
    Z-Arg-Arg-AMC hydrochloride
    		99.79%
    Z-Arg-Arg-AMC hydrochloride is a selective substrate of cathepsin B.
    Z-Arg-Arg-AMC hydrochloride
  • HY-118762
    KGP94
    		Inhibitor 99.53%
    KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines.
    KGP94
  • HY-10294
    Relacatib
    		Inhibitor 99.99%
    Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
    Relacatib
  • 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-156655A
    Olgotrelvir sodium
    		Inhibitor
    Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells.
    Olgotrelvir sodium
  • HY-P1759B
    N-CBZ-Phe-Arg-AMC TFA
    		99.95%
    N-CBZ-Phe-Arg-AMC (Z-FR-AMC) TFA is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes.
    N-CBZ-Phe-Arg-AMC TFA
  • 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-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-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-15958
    VBY-825
    		Inhibitor 99.81%
    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
    VBY-825
  • HY-112711
    LV-320
    		Inhibitor
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
    LV-320
  • 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-P2498A
    Cathepsin D and E FRET Substrate acetate
    		99.12%
    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-N2905
    Aurantiamide acetate
    		Inhibitor 99.60%
    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-17541
    Cysteine Protease inhibitor
    		Inhibitor
    Cysteine Protease inhibitor is an inhibitor of cysteine protease.
    Cysteine Protease inhibitor
  • 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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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