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Proteasome

Proteasome inhibitors block the 26S proteasome, the protease complex that degrades ubiquitin-tagged proteins. Its 20S core carries caspase-like, trypsin-like and chymotrypsin-like active sites on β subunits with an N-terminal threonine. In 1994, peptide aldehydes including MG-132 were shown to block degradation of most cell proteins. The same inhibitors prevented generation of peptides for major histocompatibility complex (MHC) class I molecules. Lactacystin, a Streptomyces metabolite, modifies the catalytic threonine of specific subunits. Later chemotypes include the boronates bortezomib and ixazomib and the epoxyketones carfilzomib and epoxomicin, which bind irreversibly. ONX-0914 prefers low molecular mass polypeptide 7 (LMP7), a subunit of the immunoproteasome.

3 Items

  • 20S Proteasome activator 1
    Cat. No.
    A77298
    CAS No.
    2761578-18-9

    20S Proteasome activator 1

    20S Proteasome Activator 1 is a potent activator of the 20S proteasome, demonstrating effective EC200 values of 0.3 μM, 0.7 μM, and 1.8 μM for trypsin-like, chymotrypsin-like, and caspase-like activities, respectively. This compound functions effectively within cellular environments, mitigating the accumulation of the pathogenic A53T mutant of α-synuclein. It is particularly useful for research in the context of neurodegenerative diseases, facilitating studies on proteostasis and related therapeutic approaches.

    In stock View Details
    5 mg
    $50.00
    10 mg
    $80.00
    All 5 sizes
  • Immunoproteasome activator 1
    Cat. No.
    A77318
    CAS No.
    901728-48-1

    Immunoproteasome activator 1

    Immunoproteasome Activator 1 is a selective activator of the immunoproteasome that enhances the presentation of MHC-I-bound peptides by over 100-fold. This compound functions by binding to the proteasome structural subunit PSMA1, facilitating the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes. Its significant biological activity makes it valuable for research focused on immune response modulation and antigen processing.

    In stock View Details
    1 mg
    $265.00
    All 1 sizes
  • Biotin-epoxomicin
    Cat. No.
    A77319
    CAS No.
    1334608-28-4

    Biotin-epoxomicin

    Biotin-epoxomicin is a proteasome subunit binder that serves as an affinity reagent for the identification and purification of proteasomal catalytic subunits. This compound enables the affinity purification of active subunits, facilitating their subsequent analysis via liquid chromatography-mass spectrometry (LC-MS). Biotin-epoxomicin is particularly useful in research applications focused on solid tumors, such as those derived from B16 melanoma, providing insights into proteasome function in cancer biology.

    In stock View Details
    1 mg
    $50.00
    5 mg
    $125.00
    All 3 sizes

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