Herc1 Inhibitors
Chemical inhibitors of Herc1 function primarily through the obstruction of the ubiquitin-proteasome pathway, a cellular mechanism that Herc1 utilizes to tag unwanted or damaged proteins for degradation. MG132, for instance, serves as a potent, reversible inhibitor of the proteasome, thereby preventing the degradation of proteins that Herc1 has marked with ubiquitin. This leads to an accumulation of these proteins within the cell, functionally inhibiting Herc1 by halting the typical turnover and regulation of protein levels it would normally manage. Likewise, Epoxomicin acts as a selective and irreversible proteasome inhibitor, targeting the same degradation pathway and leading to a similar inhibition of Herc1 activity by impeding the breakdown of its ubiquitinated substrates.
Lactacystin and Bortezomib both share the mechanism of proteasome inhibition, with Lactacystin binding covalently to the 20S proteasome and Bortezomib utilizing its boronic acid moiety to inhibit the 26S proteasome. These interactions result in the blockade of proteolytic functions that would typically degrade Herc1-tagged proteins. Carfilzomib, Oprozomib, and Marizomib, all irreversible proteasome inhibitors, similarly lead to the functional inhibition of Herc1 by ensuring that ubiquitinated proteins are not broken down, thereby interfering with Herc1's role in maintaining cellular proteostasis. Ixazomib, Delanzomib, and Nelfinavir bind and inhibit proteasome activity, which directly impacts Herc1's functionality by preventing the proteasomal degradation it relies on. Withaferin A, another proteasome inhibitor, functions analogously, preventing the degradation process of Herc1's target proteins. Lastly, Disulfiram is capable of inhibiting the proteasomal degradation pathway, which indirectly inhibits Herc1 by causing an accumulation of proteins that Herc1 has marked for degradation, thereby stalling the protein's regulatory activities within the cell.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 | |
MG132 is a potent, reversible, and cell-permeable proteasome inhibitor. Herc1 is known to have ubiquitin ligase activity, which tags proteins for degradation via the proteasome. By inhibiting the proteasome, MG132 can prevent the degradation of proteins ubiquitinated by Herc1, thus functionally inhibiting Herc1's role in protein turnover. | ||||||
Epoxomicin | 134381-21-8 | sc-201298C sc-201298 sc-201298A sc-201298B | 50 µg 100 µg 250 µg 500 µg | $137.00 $219.00 $449.00 $506.00 | 19 | |
Epoxomicin is a selective and irreversible proteasome inhibitor. Similar to MG132, it impedes the proteasomal degradation pathway, thereby blocking the functional activity of Herc1, as it relies on the proteasome for the execution of its ubiquitin ligase function. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
Lactacystin is a specific inhibitor of the proteasome. It covalently binds to the 20S proteasome, thereby inhibiting the degradation of proteins ubiquitinated by Herc1, which is essential for its regulatory role in protein quality control. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib is a dipeptidyl boronic acid analog that inhibits the 26S proteasome. It is known to block the proteolytic function of the proteasome, which would accumulate ubiquitinated protein substrates of Herc1, thereby inhibiting Herc1's role in proteostasis. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib is an irreversible proteasome inhibitor, which binds selectively and irreversibly to the 20S proteasome. This action prevents the proteasome from degrading proteins ubiquitinated by Herc1, functionally inhibiting Herc1's ubiquitin ligase activity. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an oral proteasome inhibitor. By binding to and inhibiting the proteasome, it would lead to an accumulation of Herc1 ubiquitinated proteins, thus inhibiting the protein degradation function of Herc1. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
Ixazomib is a small molecule proteasome inhibitor. By inhibiting the proteasome, it prevents the breakdown of proteins ubiquitinated by Herc1, thus blocking Herc1's function in the ubiquitin-proteasome pathway. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib is a proteasome inhibitor that can bind and inhibit the chymotrypsin-like activity of the proteasome, resulting in the accumulation of proteins tagged by Herc1 for degradation, thus functionally inhibiting Herc1. | ||||||
Nelfinavir | 159989-64-7 | sc-507314 | 10 mg | $168.00 | ||
Nelfinavir is known to inhibit the chymotrypsin-like activity of the proteasome. This inhibition can lead to an accumulation of proteins that Herc1 ubiquitinates, impeding Herc1's role in regulating protein degradation. | ||||||
Withaferin A | 5119-48-2 | sc-200381 sc-200381A sc-200381B sc-200381C | 1 mg 10 mg 100 mg 1 g | $130.00 $583.00 $4172.00 $20506.00 | 20 | |
Withaferin A is a steroidal lactone that has been shown to inhibit the proteasome. It would impede the degradation of Herc1's ubiquitinated protein targets, thereby inhibiting Herc1's function in protein quality control mechanisms. | ||||||