These inhibitors generally act by binding to the β subunits within the 20S core particle, leading to the inhibition of the proteasome's proteolytic functions. This results in the accumulation of polyubiquitinated proteins and can trigger apoptosis, especially in rapidly dividing cells. While these inhibitors do not directly target the α subunits, they affect the overall function of the 26S proteasome complex, of which the α subunits are a structural component.
The description of 26S Proteasome α inhibitors would be a misnomer because inhibition typically occurs at the β subunits where the proteolytic activity resides. However, the overall inhibition of the 26S proteasome can indirectly affect the function of the α subunits by disrupting the assembly and regulatory functions of the proteasome complex. The compounds listed above are examples of chemical inhibitors that indirectly impact the α subunits by their action on the proteolytic core of the proteasome.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
A boronic acid derivative that selectively and reversibly inhibits the β5 subunit of the proteasome. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
An bioavailable epoxyketone that targets the β5 subunit of the proteasome. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $60.00 $265.00 $1000.00 | 163 | |
A peptide aldehyde that reversibly inhibits the proteasome's chymotrypsin-like activity, predominantly affecting the β5 subunit. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
A natural product that irreversibly inhibits the proteasome's β-subunits by covalent modification. | ||||||
ONX 0914 | 960374-59-8 | sc-477437 | 5 mg | $245.00 | ||
An epoxyketone-based inhibitor that selectively targets the immunoproteasome subunit LMP7/β5i. | ||||||