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-P10061
    Cathepsin K inhibitor 4
    		Inhibitor
    Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively.
    Cathepsin K inhibitor 4
  • HY-158022
    CTSL/CAPN1-IN-1
    		Inhibitor
    CTSL/CAPN1-IN-1 (compound 14a) is an oral active CTSL and CAPN1 inhibitor with the IC50  values of 3.34 nM and 375.1 nM for CTSL and CAPN1, respectively. CTSL/CAPN1-IN-1 shows anticoronaviral activity and anti-inflammatory effect.
    CTSL/CAPN1-IN-1
  • HY-152222
    SPR38
    		Inhibitor
    SPR38 is a potent SARS-CoV-2 main protease inhibitor, with a Ki of 0.260 μM. SPR38 also inhibits hCatL and hCatB, with Ki values of 1.92 μM and 11.1 μM, respectively.
    SPR38
  • HY-N12129
    6,6′-Dihydroxythiobinupharidine
    		Inhibitor
    6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively.
    6,6′-Dihydroxythiobinupharidine
  • HY-146580
    Cathepsin C-IN-3
    		Inhibitor
    Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively.
    Cathepsin C-IN-3
  • HY-10290
    MK-0674
    		Inhibitor
    MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
    MK-0674
  • HY-146649
    LmCPB-IN-1
    		Inhibitor
    LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7.
    LmCPB-IN-1
  • HY-P4390
    Z-Leu-Leu-Arg-AMC
    Z-Leu-Leu-Arg-AMC is a peptide substrate of cathepsin S.
    Z-Leu-Leu-Arg-AMC
  • HY-P4369
    Z-Arg-Arg-AMC
    Z-Arg-Arg-AMC is a selective substrate of cathepsin B.
    Z-Arg-Arg-AMC
  • HY-152210
    ASPER-29
    		Inhibitor
    ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer.
    ASPER-29
  • HY-16121
    CAA-0225
    		Inhibitor
    CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites[1][2][3].
    CAA-0225
  • HY-P10117
    Cathepsin K inhibitor 5
    		Inhibitor
    Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor.
    Cathepsin K inhibitor 5
  • HY-163389
    Mpro/Cathepsin L-IN-1
    		Inhibitor
    Mpro/Cathepsin L-IN-1 (Compound 4d) is a SARS-CoV-2 Mpro/hCatL inhibitor, with Kis of 5.54 μM and 0.701 μM respectively.
    Mpro/Cathepsin L-IN-1
  • HY-136888
    MeOSuc-AAPV-CMK
    		Inhibitor
    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-P4306
    Z-Phe-Phe-Diazomethylketone
    		Inhibitor
    Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L.
    Z-Phe-Phe-Diazomethylketone
  • HY-P1315
    Papain inhibitor
    		Inhibitor
    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-161596
    SmCB1-IN-1
    		Inhibitor
    SmCB1-IN-1 (Compound 2h) is an inhibitor for S. mansoni cathepsin B1 (SmCB1) with an Ki of 0.05 μM. SmCB1-IN-1 exhibits selectivity toward human off-target cathepsins (29% and 37% inhibition for CatB and CatL at 20 μM). SmCB1-IN-1 inhibits 68% Schistosoma mansoni at 1 μM.
    SmCB1-IN-1
  • HY-120709
    GSK2793660 hydrochloride
    		Inhibitor
    GSK2793660 hydrochloride is an orally active, irreversible cathepsin C (CTSC) inhibitor for bronchodilation studies.
    GSK2793660 hydrochloride
  • HY-161244
    FGA145
    		Inhibitor
    FGA145 is a dual, selective inhibitor for Mpro and human Cathepsin L, with Kis of 3.71 μM, 9.82 μM and 53 nM, for Mal-Mpro, pET21-Mpro and Cathepsin L, respectively. FGA145 reveals a multitarget effects in the antiviral activity.
    FGA145
  • HY-155611
    Cathepsin C-IN-6
    		Inhibitor
    Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase，exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.，chronic obstructive pulmonary disease).
    Cathepsin C-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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