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-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-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-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-P4217
    Z-Gly-Pro-Arg-AMC hydrochloride
    		Inhibitor 98.60%
    Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsin K activity.
    Z-Gly-Pro-Arg-AMC hydrochloride
  • 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-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-144813
    Gü2602
    		Inhibitor 98.13%
    Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
    Gü2602
  • 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-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-U00377
    Cathepsin Inhibitor 2
    		Inhibitor 98.05%
    Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
    Cathepsin Inhibitor 2
  • HY-50887
    L-873724
    		Inhibitor 98.93%
    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
    L-873724
  • 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-Y0241
    2-Cyanopyrimidine
    		Inhibitor 99.92%
    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
  • 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-138208
    Z-Phe-Tyr(tBu)-diazomethylketone
    		Inhibitor ≥99.0%
    Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection.
    Z-Phe-Tyr(tBu)-diazomethylketone
  • HY-147774
    Cathepsin K inhibitor 6
    		Inhibitor 98.18%
    Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC50 of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC50s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively.
    Cathepsin K inhibitor 6
  • HY-D1634
    Bz-FVR-AMC
    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
  • HY-112318
    GSK-2793660 free base
    		Inhibitor
    GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis.
    GSK-2793660 free base
  • HY-P1759
    N-CBZ-Phe-Arg-AMC
    		99.88%
    N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes.
    N-CBZ-Phe-Arg-AMC
  • HY-103353A
    SID 26681509 quarterhydrate
    		Inhibitor
    SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G.
    SID 26681509 quarterhydrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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