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.

Items 1-25 of 130

  • MG-132
    Cat. No.
    A11043

    MG-132

    Synonyms: Z-Leu-Leu-Leu-CHO; Z-LLL-CHO

    MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).

    5 mg
    $20.00
    10 mg
    $30.00
    All 8 sizes
  • Bortezomib
    Cat. No.
    A10160

    Bortezomib (Velcade)

    Synonyms: MG-341; PS-341; Velcade

    Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome

    5 mg
    $25.00
    10 mg
    $45.00
    All 8 sizes
  • Carfilzomib
    Cat. No.
    A11278

    Carfilzomib (PR-171)

    Synonyms: PR-171-007; PR-171

    PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.

    5 mg
    $40.00
    10 mg
    $60.00
    All 7 sizes
  • ONX-0914
    Cat. No.
    A12653

    ONX-0914

    Synonyms: PR-957

    ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome.

    1 mg
    $40.00
    5 mg
    $115.00
    All 7 sizes
  • Ixazomib
    Cat. No.
    A10600

    Ixazomib (MLN2238)

    Synonyms: MLN2238

    MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.

    1 mg
    $35.00
    5 mg
    $85.00
    All 8 sizes
  • Epoxomicin
    Cat. No.
    A12730

    Epoxomicin

    Synonyms: BU-4061T

    Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.

    1 mg
    $115.00
    2 mg
    $215.00
    All 9 sizes
  • Lactacystin
    Cat. No.
    A12768

    Lactacystin

    Lactacystin is a cell-permeable, potent and selective proteasome inhibitor.

    50 µg
    $80.00
    100 µg
    $140.00
    All 6 sizes
  • Marizomib
    Cat. No.
    A13853

    Marizomib (NPI-0052, salinosporamide A)

    Synonyms: ML 858; NPI 0052; Salinosporamide A

    Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.

    100 µg
    $145.00
    500 µg
    $405.00
    All 5 sizes
  • Ixazomib Citrate (MLN9708) Analogue
    Cat. No.
    A10602

    Ixazomib Citrate (MLN9708) Analogue

    Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

    5 mg
    $35.00
    10 mg
    $55.00
    All 8 sizes
  • Delanzomib
    Cat. No.
    A11145

    Delanzomib (CEP-18770)

    Synonyms: CEP18770

    CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition.

    1 mg
    $30.00
    5 mg
    $65.00
    All 8 sizes
  • MG-115
    Cat. No.
    A11601

    MG-115

    Synonyms: Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal; Z-LL-Nva-CHO; Proteasome Inhibitor XII,MG115

    MG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis.

    1 mg
    $40.00
    5 mg
    $90.00
    All 7 sizes
  • 18α-Glycyrrhetinic acid
    Cat. No.
    A12199

    18α-Glycyrrhetinic acid

    Synonyms: 18α-GA

    18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1).

    10 mg
    $25.00
    25 mg
    $35.00
    All 4 sizes
  • MG-262
    Cat. No.
    A12220

    MG-262

    Synonyms: PS-III

    MG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome.

    200 µg
    $740.00
    1 mg
    $2,500.00
    All 2 sizes
  • RA190
    Cat. No.
    A12287

    RA190

    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

    1 mg
    $45.00
    5 mg
    $110.00
    All 7 sizes
  • VR23
    Cat. No.
    A13650

    VR23

    VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3uM).

    5 mg
    $30.00
    10 mg
    $40.00
    All 7 sizes
  • Gliotoxin
    Cat. No.
    A13711

    Gliotoxin

    Synonyms: Aspergillin; S.N. 12870

    Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi.

    1 mg
    $135.00
    5 mg
    $400.00
    All 4 sizes
  • PSI
    Cat. No.
    A14048

    PSI

    PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome.

    1 mg
    $80.00
    5 mg
    $250.00
    All 6 sizes
  • PI-1840
    Cat. No.
    A14146

    PI-1840

    PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.

    5 mg
    $30.00
    10 mg
    $55.00
    All 7 sizes
  • Oprozomib
    Cat. No.
    A14181

    Oprozomib (ONX 0912)

    Synonyms: ONX-0912

    ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies.

    1 mg
    $50.00
    5 mg
    $100.00
    All 7 sizes
  • Aclacinomycin A
    Cat. No.
    A14910

    Aclacinomycin A

    Synonyms: Jaclacin; Aclarubicin

    Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity.

    1 mg
    $180.00
    5 mg
    $460.00
    All 5 sizes
  • AM 114
    Cat. No.
    A14922

    AM 114

    AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins.

    5 mg
    $25.00
    10 mg
    $40.00
    All 7 sizes
  • Clasto-Lactacystin b-lactone
    Cat. No.
    A15427

    Clasto-Lactacystin b-lactone

    Synonyms: Omuralide

    Clasto-lactacystin b-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive b-lactone.

    0.2 mg
    $200.00
    0.5 mg
    $400.00
    All 3 sizes
  • Ixazomib citrate
    Cat. No.
    A18017

    Ixazomib citrate (MLN9708)

    Synonyms: MLN9708

    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

    5 mg
    $35.00
    10 mg
    $55.00
    All 7 sizes

Items 1-25 of 130

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