1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cathepsin

Cathepsin

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161245
    FGA146
    Inhibitor
    FGA146 is a dual, selective inhibitor for Mpro and human Cathepsin L, with Kis of 2.19 μM, 0.96 μM and 0.87 μM, for Mal-Mpro, pET21-Mpro and Cathepsin L, respectively. FGA146 reveals an antiviral activity against SARS-CoV-2.
    FGA146
  • HY-143714
    Cathepsin K inhibitor 2
    Inhibitor
    Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).
    Cathepsin K inhibitor 2
  • HY-P4302
    Z-FK-ck
    Inhibitor
    Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner.
    Z-FK-ck
  • HY-P10065
    RKLLW-NH2
    Inhibitor
    RKLLW-NH2 is a Cathepsin L inhibitor.
    RKLLW-NH2
  • HY-P4532
    Ac-Leu-Val-Lys-Aldehyde
    Inhibitor
    Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II.
    Ac-Leu-Val-Lys-Aldehyde
  • HY-146581
    Cathepsin C-IN-4
    Inhibitor
    Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively.
    Cathepsin C-IN-4
  • HY-144812
    Gü1303
    Inhibitor
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
    Gü1303
  • HY-161342
    CTSL/CAPN1-IN-2
    Inhibitor
    CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC50 values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry.
    CTSL/CAPN1-IN-2
  • HY-123531
    JNJ 10329670
    Inhibitor
    JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a Ki value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation.
    JNJ 10329670
  • HY-RS03339
    Ctsk Rat Pre-designed siRNA Set A
    Inhibitor

    Ctsk Rat Pre-designed siRNA Set A contains three designed siRNAs for Ctsk gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Ctsk Rat Pre-designed siRNA Set A
  • HY-151524
    Cathepsin K inhibitor 3
    Inhibitor
    Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies.
    Cathepsin K inhibitor 3
  • HY-D1634A
    Bz-FVR-AMC TFA
    Bz-FVR-AMC TFA 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 TFA
  • HY-N6037R
    Gardenin B (Standard)
    Inhibitor
    Gardenin B (Standard) is the analytical standard of Gardenin B (HY-N6037). This product is intended for research and analytical applications. Gardenin B is a flavonoid isolated from Gardenia jasminoides. Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC50: 6.24 μg/mL), and Cathepsin D (IC50: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC50 values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.
    Gardenin B (Standard)
  • HY-RS03323
    Ctsb Mouse Pre-designed siRNA Set A
    Inhibitor

    Ctsb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ctsb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Ctsb Mouse Pre-designed siRNA Set A
  • HY-RS03333
    Ctse Rat Pre-designed siRNA Set A
    Inhibitor

    Ctse Rat Pre-designed siRNA Set A contains three designed siRNAs for Ctse gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Ctse Rat Pre-designed siRNA Set A
  • HY-164634
    CLIK-148
    Inhibitor
    CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.
    CLIK-148
  • HY-D1523
    Z-Arg-Arg-4MβNA triacetate
    Z-Arg-Arg-4MβNA triacetate is a cathepsin B-specific substrate and can produce fluorescent end product 4MβNA (λex = 355 nm, λem = 430 nm).
    Z-Arg-Arg-4MβNA triacetate
  • HY-P5898
    Z-Val-Val-Nle-diazomethylketone
    Inhibitor
    Z-Val-Val-Nle-diazomethylketone is a cathepsin S (CATS) inhibitor. Z-Val-Val-Nle-diazomethylketone significantly inhibits the IFNg-induced upregulation of the MHCII molecules HLA-DR and Ii-p33/35 with an increase of Ii-p10 protein level. Z-Val-Val-Nle-diazomethylketone can be used for dermatological diseases like psoriasis, atopic dermatitis and actinic keratosis research.
    Z-Val-Val-Nle-diazomethylketone
  • HY-P10118
    Cathepsin L-IN-3
    Inhibitor
    Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
    Cathepsin L-IN-3
  • HY-P11326
    Ac-FR-AFC TFA
    Substrate
    Ac-FR-AFC TFA is a Cathepsin L fluorogenic substrate (Ex=400 nm, Em=505 nm). Cathepsin L activity in cells lysates is determined by measuring cleavage of Ac-FR-AFC TFA and its cleavage occurs at the FR-AFC amide bond. Ac-FR-AFC TFA can be used for activity assays and mechanistic studies on cathepsin L.
    Ac-FR-AFC TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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