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-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-156655A
    Olgotrelvir sodium
    		Inhibitor
    Olgotrelvir (STI-1558) sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells.
    Olgotrelvir sodium
  • 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-136888
    MeOSuc-AAPV-CMK
    		Inhibitor 98.01%
    MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase.
    MeOSuc-AAPV-CMK
  • HY-P1759B
    N-CBZ-Phe-Arg-AMC TFA
    		Substrate 99.79%
    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-P4515
    Z-Phe-Arg-pNA
    		99.87%
    Z-Phe-Arg-pNA is a substrate of Cathepsin L.
    Z-Phe-Arg-pNA
  • HY-137367
    Z-Val-Val-Arg-AMC
    		99.44%
    Z-Val-Val-Arg-AMC is a fluorescent peptide substrate that can be used to test the activity of cathepsins.
    Z-Val-Val-Arg-AMC
  • HY-103352
    L-006235
    		Inhibitor 99.74%
    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-102087
    JPM-OEt
    		Inhibitor 98.99%
    JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
    JPM-OEt
  • HY-146584
    Cathepsin C-IN-5
    		Inhibitor
    Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity.
    Cathepsin C-IN-5
  • HY-17541
    Cysteine Protease inhibitor
    		Inhibitor
    Cysteine Protease inhibitor is a cysteine protease inhibitor. Cysteine Protease inhibitor can be used in immunoblotting experiments of cells or tissues.
    Cysteine Protease inhibitor
  • HY-155667A
    Z-Nle-Lys-Arg-AMC acetate
    		99.58%
    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-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-114374
    RO5461111
    		Antagonist 98.01%
    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-137841
    L-Arginine-7-amido-4-methylcoumarin hydrochloride
    		99.23%
    L-Arginine-7-amido-4-methylcoumarin (Arginine 4-methyl-7-coumarylamide) hydrochloride is a specific substrate of cathepsin H but not for cathepsins L and B.
    L-Arginine-7-amido-4-methylcoumarin hydrochloride
  • HY-W010347R
    L-Homocysteine (Standard)
    		Activator
    L-Homocysteine (Standard) is the analytical standard of L-Homocysteine. This product is intended for research and analytical applications. 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[1][2].
    L-Homocysteine (Standard)
  • HY-149482
    LN5P45
    		Inhibitor 98.68%
    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-112818
    S130
    		Inhibitor 99.43%
    S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux.
    S130
  • HY-P4295
    Z-Phe-Ala-diazomethylketone
    		Inhibitor 98.06%
    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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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