RNF152 Inhibitors
Chemical inhibitors of RNF152 can exert their effects through various mechanisms, primarily by impeding the proteasome's ability to degrade ubiquitinated proteins. Proteasome inhibitors like Velcade, MG132, Epoxomicin, Lactacystin, MLN2238, Carfilzomib, Oprozomib, Delanzomib, Marizomib, Bortezomib, and Withaferin A can indirectly inhibit RNF152 by preventing the breakdown of proteins that RNF152 has tagged for degradation. The action of Velcade, a dipeptide boronic acid derivative, leads to the accumulation of proteins within the cell, including those that have been flagged by RNF152 for proteasomal degradation. This build-up results from Velcade's ability to inhibit the 26S proteasome, a critical component in the proteolysis of ubiquitinated proteins. Another such compound, MG132, a peptide aldehyde, similarly inhibits the proteasome and calpains, leading to the accumulation of RNF152's substrates, and thus impairs RNF152's role in protein turnover.
The irreversible proteasome inhibitor Epoxomicin specifically targets the proteasome, preventing the degradation of ubiquitinated substrates and thereby inhibiting RNF152's ubiquitin ligase activity. In the same vein, Lactacystin binds irreversibly to the proteasome's catalytic site, halting the degradation process of proteins involved in RNF152's ubiquitination cycle. MLN2238, once activated, impedes the 20S proteasome, leading to a similar accumulation of RNF152's substrates. The epoxyketone-based Carfilzomib has a comparable effect, irreversibly binding to the proteasome and resulting in a buildup of substrates tagged by RNF152. Oprozomib, an oral proteasome inhibitor, and Delanzomib, a boronate proteasome inhibitor, both contribute to the accumulation of RNF152's ubiquitinated substrates by impeding their proteasomal degradation. Marizomib, by irreversibly binding to the proteasome, prevents the breakdown of RNF152's substrates, thus impairing the protein's function in maintaining protein homeostasis. Bortezomib, another boronic acid derivative, operates similarly, causing substrate accumulation that interferes with RNF152's function. Withaferin A, a steroidal lactone, inhibits the proteasomal pathway resulting in the buildup of RNF152's substrates. Lastly, Auranofin, a gold-containing compound, inhibits the proteasome, which can lead to an increase in RNF152's ubiquitinated substrates, thus hindering RNF152's activity.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $132.00 $1064.00 | 115 | |
Velcade is a dipeptide boronic acid derivative that inhibits the 26S proteasome. RNF152 is involved in the ubiquitination process which targets proteins for degradation via the proteasome. Inhibition of the proteasome by Velcade would lead to accumulation of proteins, including potentially ubiquitinated substrates of RNF152, thereby inhibiting RNF152's role in protein turnover. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG132 is a peptide aldehyde that inhibits the proteasome as well as calpains. By blocking the proteasomal degradation pathway, MG132 can lead to an accumulation of ubiquitinated proteins, which may include substrates of RNF152, thus indirectly inhibiting RNF152's function. | ||||||
Epoxomicin | 134381-21-8 | sc-201298C sc-201298 sc-201298A sc-201298B | 50 µg 100 µg 250 µg 500 µg | $134.00 $215.00 $440.00 $496.00 | 19 | |
Epoxomicin is a naturally occurring epoxyketone that acts as a potent, selective, and irreversible proteasome inhibitor. By specifically targeting the proteasome, Epoxomicin would prevent the degradation of RNF152 ubiquitinated substrates, thereby indirectly inhibiting the ubiquitin ligase activity of RNF152. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $165.00 $575.00 | 60 | |
Lactacystin is a specific inhibitor of the proteasome that irreversibly binds to the catalytic site of the proteasome. This binding inhibits the degradation of proteins, including those involved with RNF152's ubiquitination process, indirectly inhibiting RNF152 by preventing turnover of its substrates. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
MLN2238 is a proteasome inhibitor that, once converted into its active form, binds and inhibits the 20S proteasome. This inhibition can indirectly affect RNF152 by accumulating its substrates that are tagged for proteasomal degradation, thus inhibiting the protein's function. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $40.00 | ||
Carfilzomib is an epoxyketone-based proteasome inhibitor that irreversibly binds to and inhibits the proteasome. The inhibition of the proteasome would lead to a buildup of RNF152's ubiquitinated substrates, indirectly inhibiting RNF152's role in the ubiquitin-proteasome pathway. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an oral proteasome inhibitor that, by inhibiting the proteasomal activity, would cause an accumulation of ubiquitinated proteins, including those tagged by RNF152, thus indirectly inhibiting RNF152's function in protein degradation. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib is a boronate proteasome inhibitor that would lead to an accumulation of ubiquitinated substrates of RNF152 by inhibiting their degradation, thereby indirectly inhibiting RNF152's ubiquitin ligase activity. | ||||||
Withaferin A | 5119-48-2 | sc-200381 sc-200381A sc-200381B sc-200381C | 1 mg 10 mg 100 mg 1 g | $127.00 $572.00 $4090.00 $20104.00 | 20 | |
Withaferin A is a steroidal lactone that has been shown to inhibit the proteasomal pathway. By inhibiting the proteasome, Withaferin A would result in the buildup of ubiquitinated substrates of RNF152, indirectly inhibiting the protein's function. | ||||||
Auranofin | 34031-32-8 | sc-202476 sc-202476A sc-202476B | 25 mg 100 mg 2 g | $150.00 $210.00 $1899.00 | 39 | |
Auranofin is a gold-containing compound that inhibits the proteasome indirectly. This inhibition can lead to an increase in ubiquitinated substrates, which could include those of RNF152, thereby inhibiting RNF152's activity by preventing its substrates from being degraded. | ||||||