20S Proteasome α3 Inhibitors
The class of 20S Proteasome α3 inhibitors presents a diverse repertoire of chemicals that intricately modulate the functional activity of the 20S proteasome α3 subunit. Within this category, Bortezomib and Carfilzomib emerge as direct inhibitors, binding to the β5 subunit of the proteasome. By doing so, they not only inhibit proteasomal activity but also induce apoptosis. Expanding the scope, MG-132, ONX-0914, Delanzomib, Marizomib, Oprozomib, KZR-616, and PR-924 exhibit their inhibitory effects by targeting specific catalytic sites within the 20S proteasome. Whether acting directly or indirectly, these inhibitors disrupt proteasome activity, contributing to the disruption of cellular protein homeostasis. Ginkgolic Acid offers a unique perspective, showcasing reversible inhibition, adding a layer of intricacy to the array of inhibitory mechanisms.
The indirect modulation of the 20S proteasome is exemplified by Ritonavir and Celastrol. These compounds underscore the multifaceted nature of proteasome regulation, influencing its activity through pathways that extend beyond direct binding to catalytic sites. Collectively, this array of inhibitors contributes significantly to our understanding of the intricate network governing cellular protein turnover. In essence, the multifaceted mechanisms employed by these inhibitors highlight the complexity of proteasomal regulation. Their diverse modes of action, from direct binding to catalytic sites to indirect modulation of cellular pathways, enrich our understanding of the intricate processes governing protein homeostasis.
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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 is a reversible proteasome inhibitor that specifically targets the 20S proteasome. It binds to the catalytic site of the β5 subunit of the 20S proteasome, preventing its activity. This direct inhibition leads to the accumulation of ubiquitinated proteins and induces cell apoptosis. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib is a second-generation proteasome inhibitor that irreversibly binds to the β5 subunit of the 20S proteasome. By forming a covalent bond with the active site, Carfilzomib inhibits proteasomal activity, resulting in the accumulation of misfolded proteins and cell death. The irreversible nature of this inhibition provides a sustained effect on the 20S 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 | |
MG-132 is a reversible and selective proteasome inhibitor that directly targets the catalytic sites of the 20S proteasome subunits, including α3. By blocking the proteolytic activity of the 20S proteasome, MG-132 leads to the accumulation of ubiquitinated proteins, affecting cellular processes and promoting apoptosis. | ||||||
ONX 0914 | 960374-59-8 | sc-477437 | 5 mg | $245.00 | ||
ONX-0914 is a selective immunoproteasome inhibitor that specifically targets the β5i subunit of the 20S proteasome. By inhibiting immunoproteasome activity, ONX-0914 can indirectly influence the 20S proteasome α3 subunit's function. This inhibition alters the cellular protein degradation landscape, affecting processes reliant on proteasomal activity and contributing to cytotoxic effects. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib is a proteasome inhibitor that selectively targets the β5 subunit of the 20S proteasome. Its direct binding to the catalytic site inhibits proteasomal activity, resulting in the accumulation of polyubiquitinated proteins. This accumulation disrupts cellular homeostasis, triggering apoptosis. Delanzomib's specificity for the β5 subunit ensures selective modulation of the 20S proteasome. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is a reversible proteasome inhibitor that targets the β5 subunit of the 20S proteasome. By binding to the catalytic site, Oprozomib inhibits proteasomal activity and induces the accumulation of ubiquitinated proteins. | ||||||
Ginkgolic acid C17:1 | 111047-30-4 | sc-228252 sc-228252A sc-228252B | 5 mg 10 mg 20 mg | $285.00 $461.00 $851.00 | 2 | |
Ginkgolic Acid inhibits the 20S proteasome by directly binding to its catalytic sites. It induces a reversible inhibition of proteasomal activity, leading to the accumulation of ubiquitinated proteins. | ||||||
Ritonavir | 155213-67-5 | sc-208310 | 10 mg | $124.00 | 7 | |
Ritonavir is a HIV protease inhibitor that indirectly impacts the 20S proteasome. It alters the ubiquitin-proteasome system by affecting the turnover of proteasome regulatory particles. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol inhibits the 20S proteasome by directly interacting with its catalytic sites. This direct inhibition leads to the accumulation of ubiquitinated proteins, affecting cellular processes and promoting apoptosis. | ||||||