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-139111
    Oxocarbazate
    		Inhibitor
    Oxocarbazate is an inhibitor of human cathepsin L with the IC50 values of 6.9 nM (human Cathepsin L,0 h) 0.4 nM ((human Cathepsin L,4 h) and 5.07 μM (human cathepsin B), respectively. Oxocarbazate blockes both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into 293T cells.
    Oxocarbazate
  • HY-118959
    S2160
    S2160 is a substrate of Cathepsin B that can be utilized in the calorimetric assay for the measurement of cathepsin B.
    S2160
  • HY-124202
    SQ 32602
    		Inhibitor
    SQ 32602 is an inhibitor of cathepsin E, with the IC50 of 88 nM.
    SQ 32602
  • HY-169171
    Cathepsin L-IN-5
    		Inhibitor
    Cathepsin L-IN-5 (D6-3) is a potent Cathepsin L (CatL) inhibitor with an IC50 of 0.27 nM. Cathepsin L-IN-5 effectively blocks the CatL function and substantially hinders the entry of the SARS-CoV-2 pseudovirus to cells by inhibiting the cleavage of the spike protein. Cathepsin L-IN-5 can be utilized in SARS-CoV-2 research.
    Cathepsin L-IN-5
  • HY-15099
    NC 2300
    		Inhibitor
    NC 2300 (VEL-0230)is a selective and orally active cysteine cathepsin inhibitor with the IC50 values of 284, 34.5, and 186 nM for cathepsin B, K, and S, respectively.NC 2300 can be used for study of diseases involving bone mineral disorders.
    NC 2300
  • HY-164958
    TB-11
    		Inhibitor
    TB-11 is a Cathepsin D inhibitor, with IC50s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research.
    TB-11
  • HY-129461
    Dibenzyl trisulfide
    		Inducer
    Dibenzyl trisulfide (DTS) is an active ingredient that can be isolated from Petiveria alliacea L.. Dibenzyl trisulfide inhibits cell proliferation and migration. Dibenzyl trisulfide decreased the mRNA and protein expression of BAK-1 and LTA. Dibenzyl trisulfide induces lysosomal membrane permeabilization and cathepsin B release.
    Dibenzyl trisulfide
  • HY-Y0241R
    2-Cyanopyrimidine (Standard)
    		Inhibitor
    2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos.
    2-Cyanopyrimidine (Standard)
  • HY-163029
    CTSL/B-IN-1
    		Inhibitor
    CTSLCTSB-IN-1 (compound 212-148) is a bispecific inhibitor of host viral spike cleaver proteins CTSL/CTSB and TMPRSS2 with IC50s of 2.13/64.07 nM and 1.38 μM, respectively. CTSLCTSB-IN-1 blocks two relevant SARS-CoV-2 viral entry pathways by inhibiting the viral spike cleavage and can be applied to anti-SARS-CoV-2 research.
    CTSL/B-IN-1
  • HY-170819
    VK13
    		Inhibitor
    VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) with a Ki value of 0.55 nM and SARS-CoV-2 3CLpro (3CL-PR) with a Ki value of 2.6 nM. VK13 exhibits anti-CoV-2 activity with an EC50 of 1.25 μM.
    VK13
  • HY-163206
    SARS-CoV-2-IN-77
    		Inhibitor
    SARS-CoV-2-IN-77 (compound 11e) is a cathepsin L and cathepsin S inhibitor with Ki values of 111 nM and 103 nM, respectively. SARS-CoV-2-IN-77 inhibits SARS-CoV-2 with an EC50 value of 38.4 nM in Calu-3 cells without showing cytotoxicity.
    SARS-CoV-2-IN-77
  • HY-158763
    MPI8
    		Inhibitor
    MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19.
    MPI8
  • HY-N14193
    Estatin B
    		Inhibitor
    Estatin B is a thiol protease inhibitor found by the Thermophilic Bacterium M4323, which is specific to thiol proteases such as papain, fig protease, and bromelain. Estatin B inhibits the production of IgE antibodies but not IgG in mice.
    Estatin B
  • HY-123185
    (Rac)-Z-FA-FMK
    		Inhibitor
    (Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.
    (Rac)-Z-FA-FMK
  • HY-176229
    Mpro/Cathepsin L-IN-2
    		Inhibitor
    Mpro/Cathepsin L-IN-2 (Compound 1) is a dual irreversible inhibitor of SARS-CoV-2 main protease (Mpro, pIC50=8.61) and human cathepsin L (hCTSL, pIC50=7.64). Mpro/Cathepsin L-IN-2 is promising for research of COVID-19 and other coronavirus infections.
    Mpro/Cathepsin L-IN-2
  • HY-103352R
    L-006235 (Standard)
    		Inhibitor
    L-006235 (Standard) is the analytical standard of L-006235. This product is intended for research and analytical applications. 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 (Standard)
  • HY-113721
    BML-244
    		Inhibitor
    BML-244 is a potent cathepsin K inhibitor. BML-244 can be used in the study of rheumatoid arthritis (RA) and periodontitis.
    BML-244
  • HY-100223R
    Calpeptin (Standard)
    		Inhibitor
    Calpeptin (Standard) is the analytical standard of Calpeptin. This product is intended for research and analytical applications. Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
    Calpeptin (Standard)
  • HY-100229R
    Aloxistatin (Standard)
    		Inhibitor
    Aloxistatin (Standard) is the analytical standard of Aloxistatin. This product is intended for research and analytical applications. Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
    Aloxistatin (Standard)
  • HY-N14403
    6-Hydroxytetrangulol
    		Activator
    6-Hydroxytetrangulol is a CPP32 protease inducer found in Streptomyces sp.
    6-Hydroxytetrangulol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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