Cathepsin

Cathepsin inhibitors act on lysosomal proteases, mainly the papain-like cysteine cathepsins B, C, K, L and S. Cysteine cathepsins degrade proteins in the endolysosomal system and, after secretion, also remodel the extracellular matrix. In 1996 loss of cathepsin K was shown to cause pycnodysostosis, a lysosomal disease with dense, brittle bones. Cathepsin K is the main collagen-degrading protease of osteoclasts, which makes it a target in bone resorption studies. Odanacatib and balicatib inhibit cathepsin K, petesicatib targets cathepsin S, and CA-074 is selective for cathepsin B. CA-074 methyl ester is a membrane-permeable form for work in intact cells. Gly-Phe-beta-naphthylamide, a cathepsin C substrate, is used to rupture lysosomes in live cells.

Items 1-25 of 88

  • CA-074 Methyl Ester
    Cat. No.
    A13593

    CA-074 Methyl Ester

    Synonyms: CA-074 Me

    CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.

    1 mg
    $45.00
    2 mg
    $65.00
    All 8 sizes
  • CA-074
    Cat. No.
    A13256

    CA-074

    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

    1 mg
    $65.00
    5 mg
    $190.00
    All 7 sizes
  • VBY-825
    Cat. No.
    A21069

    VBY-825

    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.

    1 mg
    $270.00
    2 mg
    $405.00
    All 7 sizes
  • Cathepsin Inhibitor 1
    Cat. No.
    A11466

    Cathepsin Inhibitor 1

    Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

    1 mg
    $35.00
    5 mg
    $90.00
    All 8 sizes
  • Balicatib
    Cat. No.
    A12020

    Balicatib

    Synonyms: AAE581; AAE-581,AAE 581

    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys.

    2 mg
    $30.00
    5 mg
    $50.00
    All 8 sizes
  • L-873724
    Cat. No.
    A12487

    L-873724

    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor.

    1 mg
    $720.00
    5 mg
    $1,550.00
    All 4 sizes
  • Pepstatin A
    Cat. No.
    A14262

    Pepstatin A

    Synonyms: Pepstation-A

    Pepstatin A is a potent aspartic protease inhibitor, and also inhibits HIV replication.

    5 mg
    $25.00
    10 mg
    $40.00
    All 7 sizes
  • L 006235
    Cat. No.
    A15302

    L 006235

    L006235 is a potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S.

    2 mg
    $30.00
    5 mg
    $50.00
    All 8 sizes
  • SID 26681509
    Cat. No.
    A15313

    SID 26681509

    SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G.

    1 mg
    $55.00
    5 mg
    $140.00
    All 7 sizes
  • LY3000328
    Cat. No.
    A15685

    LY3000328

    LY3000328 is a Cathepsin S inhibitor with excellent in vitro potency and selectivity against other cysteine proteases.

    1 mg
    $90.00
    2 mg
    $130.00
    All 8 sizes
  • MIV-247
    Cat. No.
    A20122

    MIV-247

    MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

    1 mg
    $250.00
    2 mg
    $450.00
    All 7 sizes
  • MK-0674
    Cat. No.
    A21558

    MK-0674

    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.

    1 mg
    $315.00
    2 mg
    $600.00
    All 6 sizes
  • Oxocarbazate
    Cat. No.
    A22503

    Oxocarbazate

    Synonyms: CID 23631927

    Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L.

    5 mg
    $115.00
    10 mg
    $215.00
    All 5 sizes
  • Z-FY-CHO
    Cat. No.
    A24230

    Z-FY-CHO (Z-Phe-Tyr-CHO)

    Synonyms: Z-Phe-Tyr-CHO

    Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific inhibitor of cathepsin L (CTSL), a lysosomal cysteine protease involved in protein degradation and various pathological processes. It is commonly used as a tool compound in studies of CTSL-related functions and diseases.

    5 mg
    $81.00
    10 mg
    $140.00
    All 4 sizes
  • (Rac)-Z-FA-FMK
    Cat. No.
    A25310

    (Rac)-Z-FA-FMK

    (Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis.

    Out of stock

    All 3 sizes
  • TS-24
    Cat. No.
    A31345

    TS-24

    TS-24 is a selective inhibitor of cathepsin S, demonstrating an IC50 value of 4.3 μM. This compound has been shown to exhibit radiosensitizing effects in wild-type BRCA1 and triple-negative breast cancer (TNBC) xenograft models, primarily by inducing apoptotic pathways. TS-24 is suitable for research applications focused on cancer therapeutic development and understanding cathepsin-mediated biological processes.

    1 mg
    $30.00
    5 mg
    $75.00
    All 6 sizes
  • NCO-700
    Cat. No.
    A31772

    NCO-700

    NCO-700 is a potent dual inhibitor of cathepsin B and calcium-activated neutral protease (CANP), exhibiting IC50 values of 0.8 μM and 46 μM, respectively. This compound effectively reduces myocardial fibrin degradation by inhibiting protease activity and demonstrates significant anti-tumor effects on hormone-independent cancer cells, including prostate cancer, by inducing apoptosis. NCO-700 serves as a valuable tool for investigating mechanisms underlying myocardial ischemia and exploring novel treatments for refractory hormone-independent tumors.

    Out of stock

    All 3 sizes
  • Dual Cathepsin L/JAK-IN-1
    Cat. No.
    A33315

    Dual Cathepsin L/JAK-IN-1

    Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions.

    5 mg
    $245.00
    10 mg
    $405.00
    All 3 sizes
  • Cathepsin L-IN-6
    Cat. No.
    A36022

    Cathepsin L-IN-6

    Cathepsin L-IN-6 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 0.021 μM. It functions by directly binding to cathepsin L, effectively suppressing its enzymatic activity. Additionally, Cathepsin L-IN-6 inhibits pro-inflammatory cytokines IL-6 and IL-8, demonstrating significant anti-inflammatory properties. This compound is particularly relevant for research focused on acute lung injury and related inflammatory conditions.

    Out of stock

    All 3 sizes
  • Tasiamide B
    Cat. No.
    A37580

    Tasiamide B

    Tasiamide B is a potent inhibitor of Cathepsin D and HSP90, derived from the marine cyanobacteria Symploca sp. This linear peptide serves as a valuable scaffold for the development of inhibitors targeting aspartic proteases. Tasiamide B has demonstrated significant efficacy in skin cancer studies by effectively interacting with HSP90, highlighting its potential in cancer research and therapeutic applications.

    Out of stock

    All 3 sizes
  • LV-320
    Cat. No.
    A39447

    LV-320

    LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways.

    5 mg
    $330.00
    10 mg
    $540.00
    All 5 sizes
  • Cathepsin G Inhibitor I
    Cat. No.
    A39778

    Cathepsin G Inhibitor I

    Cathepsin G Inhibitor I is a potent and selective reversible competitive inhibitor of Cathepsin G, exhibiting an IC50 value of 53 nM and a Ki of 63 nM. This non-peptidic compound is primarily utilized in research investigating immune disorders, providing valuable insights into the role of Cathepsin G in various pathogenic processes. Its specificity makes it a useful tool for understanding the implications of Cathepsin G in immune system regulation.

    1 mg
    $95.00
    5 mg
    $245.00
    All 6 sizes

Items 1-25 of 88

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