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-15100
    Balicatib
    		Inhibitor 98.00%
    Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.
    Balicatib
  • 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
  • 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-D0843S
    N-Ethylmaleimide-d5
    		Inhibitor 99.49%
    N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
    N-Ethylmaleimide-d<sub>5</sub>
  • HY-P3042
    Chymostatin
    		Inhibitor ≥99.0%
    Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research.
    Chymostatin
  • HY-115733
    Cathepsin L-IN-2
    		Inhibitor 98.27%
    Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor.
    Cathepsin L-IN-2
  • HY-109069
    Petesicatib
    		Inhibitor 99.71%
    Petesicatib (RO5459072; RG-7625) is a cathepsin S inhibitor, used in research of immune diseases.
    Petesicatib
  • HY-146985
    Cathepsin X-IN-1
    		Inhibitor 98.81%
    Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic.
    Cathepsin X-IN-1
  • HY-108137
    Z-LVG-CHN2
    		Inhibitor 99.88%
    Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease.
    Z-LVG-CHN2
  • HY-103351
    Cathepsin G Inhibitor I
    		Inhibitor ≥99.0%
    Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
    Cathepsin G Inhibitor I
  • HY-128971
    LHVS
    		Inhibitor 99.87%
    LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM.
    LHVS
  • 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-112318A
    GSK-2793660
    		Inhibitor 99.66%
    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-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-P0111
    Z-WEHD-FMK
    		Inhibitor ≥98.0%
    Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
    Z-WEHD-FMK
  • HY-102087
    JPM-OEt
    		Inhibitor 99.06%
    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-118355
    ALLM
    		Inhibitor ≥98.0%
    ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
    ALLM
  • HY-P4373A
    Hepcidin-1 (mouse) (TFA)
    		Inducer 98.94%
    Hepcidin-1 (mouse) TFA is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) TFA upregulates mRNA levels of TRAP, cathepsin K, and MMP-9 and increases TRAP-5b protein secretion. Hepcidin-1 (mouse) TFA downregulates the level of FPN1 protein and increases intracellular iron. Hepcidin-1 (mouse) TFA facilitates osteoclast differentiation.
    Hepcidin-1 (mouse) (TFA)
  • 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-W011063
    Gly-Phe-β-naphthylamide
    		99.87%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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