20S Proteasome α7 Inhibitors
The class of 20S Proteasome α7 inhibitors comprises a set of chemically diverse compounds strategically designed to modulate the catalytic activity of the proteasome, specifically targeting the α7 subunit. Bortezomib, one of the prominent inhibitors in this class, exerts its inhibitory effects by reversibly binding to the catalytic site of 20S Proteasome α7, preventing chymotrypsin-like activity. This binding leads to the accumulation of misfolded or ubiquitinated proteins, inducing cell cycle arrest and apoptosis in susceptible cells. Carfilzomib, another member of this class, irreversibly binds to the active site of 20S Proteasome α7, selectively inhibiting chymotrypsin-like activity. This irreversible binding disrupts the normal protein degradation process, resulting in the accumulation of misfolded or ubiquitinated proteins. Ixazomib, Oprozomib, and MLN2238 share a similar mechanism, with reversible binding to the catalytic site, inhibiting chymotrypsin-like activity and triggering cell cycle arrest and apoptosis.
Delanzomib, while also targeting chymotrypsin-like activity, exerts its inhibitory effects through reversible binding. Marizomib and ONX-0914 selectively inhibit chymotrypsin-like activity by binding to the catalytic site, disrupting proteolytic degradation. Nelfinavir, an antiretroviral drug, induces proteasome inhibition, leading to the accumulation of misfolded proteins and cell death. Gliotoxin and Betulinic Acid, though differing in structure, both form covalent complexes with the proteasome, particularly affecting chymotrypsin-like activity. Celastrol disrupts the chymotrypsin-like activity, preventing normal protein degradation. The class collectively represents a nuanced approach to selectively modulate 20S Proteasome α7 activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib inhibits 20S Proteasome α7 by reversibly binding to the catalytic site of the proteasome, preventing the chymotrypsin-like activity. This inhibition leads to the accumulation of misfolded or ubiquitinated proteins, triggering cell cycle arrest and apoptosis in susceptible cells. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib inhibits 20S Proteasome α7 by irreversibly binding to its active site. This binding selectively inhibits chymotrypsin-like activity, disrupting the normal protein degradation process. The resulting accumulation of misfolded or ubiquitinated proteins induces cellular stress, leading to apoptosis and growth inhibition in targeted cells. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
Ixazomib inhibits 20S Proteasome α7 by reversible binding to the catalytic site, selectively inhibiting the chymotrypsin-like activity. This inhibition disrupts the proteolytic degradation of key cellular proteins, triggering cell cycle arrest and apoptosis. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib inhibits 20S Proteasome α7 by irreversibly binding to its catalytic site. This binding specifically inhibits the chymotrypsin-like activity, disrupting the proteasomal degradation process. The resulting accumulation of misfolded or ubiquitinated proteins induces cellular stress, leading to apoptosis and growth inhibition in targeted cells. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib inhibits 20S Proteasome α7 by reversible binding to its catalytic site, selectively inhibiting the chymotrypsin-like activity. This inhibition disrupts the normal protein degradation process, leading to the accumulation of misfolded or ubiquitinated proteins. The ensuing cellular stress triggers apoptosis and growth inhibition in susceptible cells. | ||||||
ONX 0914 | 960374-59-8 | sc-477437 | 5 mg | $245.00 | ||
ONX-0914 inhibits 20S Proteasome α7 by selectively binding to its active site, specifically inhibiting the chymotrypsin-like activity. This inhibition disrupts the normal protein degradation process, leading to the accumulation of misfolded or ubiquitinated proteins. The ensuing cellular stress triggers apoptosis and growth inhibition in susceptible cells. | ||||||
Nelfinavir | 159989-64-7 | sc-507314 | 10 mg | $168.00 | ||
Nelfinavir inhibits 20S Proteasome α7 through a mechanism involving the disruption of proteasomal function. The precise details of the interaction are not fully elucidated, but studies suggest that Nelfinavir induces proteasome inhibition, leading to the accumulation of misfolded or ubiquitinated proteins and subsequent cell death in susceptible cells. | ||||||
Gliotoxin | 67-99-2 | sc-201299 sc-201299A | 2 mg 10 mg | $134.00 $394.00 | 1 | |
Gliotoxin inhibits 20S Proteasome α7 by forming a covalent complex with the proteasome, particularly affecting its chymotrypsin-like activity. This covalent binding disrupts the normal protein degradation process, leading to the accumulation of misfolded or ubiquitinated proteins. The resulting cellular stress triggers apoptosis and growth inhibition in targeted cells. | ||||||
Betulinic Acid | 472-15-1 | sc-200132 sc-200132A | 25 mg 100 mg | $117.00 $344.00 | 3 | |
Betulinic Acid inhibits 20S Proteasome α7 through a mechanism involving the inhibition of the chymotrypsin-like activity. This disruption of proteasomal function leads to the accumulation of misfolded or ubiquitinated proteins, inducing cellular stress and triggering apoptosis and growth inhibition in susceptible cells. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol inhibits 20S Proteasome α7 by disrupting the chymotrypsin-like activity of the proteasome. This disruption prevents the normal degradation of cellular proteins, leading to the accumulation of misfolded or ubiquitinated proteins. The resulting cellular stress triggers apoptosis and growth inhibition in susceptible cells. | ||||||