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Ubiquitin/Proteasome

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  • Aclacinomycin A | 57576-44-0 | Structure | Supplier
    $75.00
    Aclacinomycin A HCl (75443-99-1) is a specific inhibitor of the 20S proteasome chymotrypsin-like activity.1 Inhibition of Brg1 proteasomal degradation by aclacinomycin A reverses (0.25 μM in ILU-18 cells ) the removal of...

  • b-AP15 | 1009817-63-3 | Structure | Supplier
    $60.00
    b-AP15 (1009817-63-3) abrogates the deubiquitinating activity of the 19S regulatory particle by inhibiting ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14) resulting in accumulation of...

  • Bortezomib | Proteasome inhibitor
    $50.00
    Potent and selective proteasome inhibitor (Ki=0.6 nM). Inhibits proliferation of a number of tumor cell lines (IC50=7 nM).  Inhibits TNFα synthesis and FGF-induced angiogenesis. Clinically useful agent for...

  • Bz-Val-Gly-Arg-AMC | Proteasome substrate
    $30.00
    Bz-VGR-AMC (87779-49-5) may be used for measuring the trypsin-like activity of the 20S proteasome, in combination with Suc-LLVY-AMC (Cat.# 10-2971, for assaying its chymotrypsin-like activity) and Z-LLE-AMC, (for determining...

  • Carfilzomib | 868540-17-4 | Structure | supplier
    $50.00
    Carfilzomib (868540-17-4) is a potent and irreversible proteasome inhibitor.1 Synthetic analog of the microbial product epoxomcin.2 Compared to bortezomib it displays equal potency but greater selectivity for the...

  • Celastrol | Proteasome inhibitor
    $116.00
    Celastrol (34157-83-0) displays potent antioxidant and anti-inflammatory activity. Inhibits NFκB (IC50=270 nM). It induces heat shock response and cytoprotection in various cells. Celastrol inhibits 20S proteasome...

  • DBeQ | 177355-84-9 | Structure | Supplier
    $65.00
    DBeQ (177355-84-9) is a potent, selective and reversible inhibitor of the AAA-ATPase p97 (ATPase associated with diverse cellular activities). Ki=3.2 μM. DBeQ blocks ubiquitin-dependent protein clearance pathways. Cell...

  • Epoxomicin | 134381-21-8 | Structure | Supplier
    $145.00
    Epoxomicin (134381-21-8) is a potent, selective and cell permeable irreversible inhibitor of the 20S proteasome.1 It does not inhibit non-proteasomal proteases such as papain, chymotrypsin, trypsin, calpain and cathepsin B...

  • Heclin | HECT domain containing E3 ubiquitin ligase inhibitor
    $60.00
    Heclin (890605-54-6) is the first small molecule inhibitor of the HECT domain-containing E3 ubiquitin ligases. Heclin (HECT ligase inhibitor) inhibits several HECT ligases in cultured cells, IC50s = 6.8, 6.3 and 6.9 μM...

  • IU1 | 314245-33-5 | Structure | Supplier
    $50.00
    IU1 (314245-33-5) is a selective inhibitor of Usp14 (IC50 < 4 μM). Enhances proteasome activity and substrate proteolysis. Cell permeable. References/Citations1) Lee et al. (2010), Enhancement of proteasome activity...

  • Lactacystin | 133343-34-7 | Structure | Supplier
    $126.00
    Lactacyctin (133343-34-7) is a specific inhibitor of three proteolytic activities of the proteasome. Chymotrypsin-like activity is inhibited most potently followed by trypsin-like activity. Inhibition of the...

  • LDN-57444 | 668467-91-2 | Structure | Supplier
    $90.00
    LDN-57444 (668467-91-2) inhibits ubiquitin C-terminal hydrolase (UCH-L1) (Ki=0.4 μM). Decreases proteasome activity and increases levels of ubiquitinated proteins. Induces apoptosis. LDN-57444 causes dramatic alterations...

  • Lenalidomide | Immunomodulator
    $50.00
    Lenalidomide (191732-72-6) is a thalidomide analog which, like thalidomide1, binds to cereblon which is the substrate recognition component of a cullin-dependent ubiquitin ligase and inhibits its autoubiquitination activity2...

  • MDBN | 1485-00-3 | Structure | Supplier
    $40.00
    MDBN (1485-00-3) is an irreversible inhibitor of p97 (IC50 < 10 μM). Cell permeable References/Citations1) Chou et al. (2011), Quantitative cell-based protein degradation assays to identify and classify drugs that...

  • MG-132 | 133407-82-6 | Structure | Supplier
    $50.00
    MG-132 (133407-82-6) is a specific inhibitor of the chymotrypsin-like activity of the 20S proteasome (IC50=100 nM with Z-LLL-AMC as substrate).1 Also inhibits calpain (IC50=1.25 μM).1 Suppresses gastric cancer cell...

  • ML-323 | USP-1/UAF-1 inhibitor
    $85.00
    ML-323 (1571424-83-5) is a potent and reversible USP1-UAF1 deubiquitinase complex inhibitor with excellent selectivity against human DUBs, deSUMOylase, deneddylase and unrelated proteases, IC50=76 nM in a ubiquitin-rhodamine...

  • MLN4924 | 905579-51-3 | Structure | Supplier
    $40.00
    MLN4924 (905579-51-3) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor. Disrupts cullin-RING ligase-mediated protein turnover leading to apoptosis in human tumor cells. Supresses the growth of tumor...

  • NSC-632839 | 157654-67-6 | Structure | Supplier
    $65.00
    NSC-632839 (157654-67-6) is a pan-specific ubiquitin isopeptidase inhibitor. (IC50= 45, 37 and 9.8 μM for USP2, USP7 and SENP2 respectively) Does not effect proteasome proteolytic activity. NSC-632839 induces apoptosis...

  • NSC-697923 | 343351-67-7 | Structure | Supplier
    $50.00
    NSC-69723 (343351-67-7) is a selective inhibitor of E2 ubiquitin-conjugating enzyme, Ubc13-Uev1A. Does not inhibit UbcH5c activity. Impedes the formation of the Ubc13 and inhibits NF-κB activation in activated B...

  • P5091 | 882257-11-6 | Structure | Supplier
    $60.00
    P5091 (882257-11-6) is a selective inhibitor of the ubiquitin-specific protease USP7 ( IC50=4.2 μM)1,2. Induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance1. P5091 displays antiangiogenic...

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