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Ubiquitination/ Proteasome

Ubiquitination is a process in targeting proteins for degradation by the proteasome. Ubiquitin (Ub) is a 76 amino acid polypeptide which can be covalently attached to various cellular proteins by the ubiquitination process. This ubiquitin-proteasome system plays a vital role in cell division, growth, differentiation, transcriptional regulation, apoptosis and immunity etc. Three main types of enzymes are involved in the process of ubiquitination. In the first step, activation of ubiquitin is carried out by ubiquitin-activating enzyme (E1) through an ATP-dependent reaction. In the second step, the activated ubiquitin is transferred from E1 to ubiquitin-conjugating enzyme (E2). In the final step, the ubiquitin protein ligase (E3) is required for labeling the ubiquitin to target substrate protein. An isopeptide bond is formed between the carboxyl terminus of ubiquitin and the ε-amino group of a lysine residue in the target protein.

Once the substrate protein is labeled, proteasome will bind to a polyubiquitin chain, allowing the degradation of the labeled protein. The polyubiquitinated target protein is then recognized and degraded by the 26S proteasome. Deubiquitinating enzymes (DUBs) reverse the process of ubiquitination by removing ubiquitin from its substrate protein. Dysregulation of the ubiquitin-proteasome system has been linked to cancer, diabetes, cardiovascular and neurodegenerative diseases etc.

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  1. CB-5083
    Catalog No. :
    B6032
    p97 inhibitor
  2. STF-62247
    Catalog No. :
    B2151
    Autophagy inducer in renal cell
    STF-62247 shows selectivtoxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
  3. Dihydroeponemycin
    Catalog No. :
    A8172
    Proteasome inhibitor,antitumor reagent,eponemycin ddrivative
    Description:IC50: 100 nm (antiproliferative IC50) [1]
  4. HMB-Val-Ser-Leu-VE
    Catalog No. :
    C4090
    inhibitor of the trypsin-like activity of the 20S proteasome
  5. C598-0466
    Catalog No. :
    A8740
    USP7 inhibitor
  6. Ubiquitin Isopeptidase Inhibitor I
    Catalog No. :
    C3250
    ubiquitin isopeptidase inhibitor
  7. VPS34-IN1
    Catalog No. :
    B6179
    Vps34 inhibitor
  8. MRT68921
    Catalog No. :
    B6174
    dual autophagy kinase ULK1/2 inhibitor
  9. PIK-III
    Catalog No. :
    B6160
    VPS34 inhibitor and inhibits autophagy
  10. ML241 hydrochloride
    Catalog No. :
    B6122
    p97 ATPase inhibitor

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