RNF180 Inhibitors
Chemical inhibitors of RNF180 function by interfering with the protein degradation pathways it typically utilizes. Proteasome inhibitors such as MG132, Bortezomib (also known by its trade name Velcade), Lactacystin, Epoxomicin, MLN2238, Carfilzomib, Marizomib, Oprozomib, and Delanzomib operate by directly targeting the proteasome, a complex responsible for degrading ubiquitinated proteins. MG132 achieves this inhibition by reversible binding, while Lactacystin and Marizomib irreversibly bind to the proteasome's catalytic site. Bortezomib and its analog MLN2238 preferentially inhibit the β5 subunit of the 20S proteasome. Epoxomicin selectively binds to the chymotrypsin-like activity of this complex, and Carfilzomib, like Marizomib, forms an irreversible bond. These inhibitors cause an accumulation of proteins that RNF180 has tagged for degradation, which leads to a functional bottleneck in the protein's activity.
On the other hand, Chloroquine works through a different mechanism. It raises the pH within cellular vesicles like lysosomes, which are also involved in protein degradation, albeit less specifically than the proteasome. By altering the lysosomal pH, Chloroquine interferes with the degradation of proteins within these organelles, which can indirectly affect the functional role of RNF180. Similarly, Nelfinavir, although primarily known for its antiviral properties, has been shown to exert an inhibitory effect on the proteasome. The inhibition of these pathways by the aforementioned compounds results in the buildup of ubiquitinated proteins within the cell. This buildup indicates a functional inhibition of RNF180, as the protein cannot complete its role in the cellular mechanism that recycles proteins, maintaining cellular homeostasis.
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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 proteasome inhibitor that can prevent the degradation of ubiquitinated proteins. Because RNF180 is an E3 ubiquitin-protein ligase, MG132's inhibition of the proteasome would lead to the accumulation of RNF180's substrates, thereby functionally inhibiting RNF180's role in targeting proteins for degradation. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Chloroquine is known to raise the pH of acidic vesicles within cells, such as lysosomes. By increasing lysosomal pH, it can inhibit the degradation of proteins inside lysosomes. Since RNF180 is implicated in pathways that involve protein degradation, chloroquine's function could result in the functional inhibition of RNF180 by disrupting the degradation process of its substrates. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib is a dipeptide boronic acid analogue that inhibits the 26S proteasome. Since RNF180 functions as an E3 ligase targeting proteins for proteasomal degradation, bortezomib's proteasome inhibition would impair the degradation pathway of RNF180's substrates, thereby inhibiting RNF180's 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. By irreversibly binding to the proteasome's catalytic site, it can inhibit the degradation of polyubiquitinated proteins, which would otherwise be mediated by E3 ligases like RNF180, leading to functional inhibition of RNF180. | ||||||
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 proteasome inhibitor. It covalently binds to and inhibits the chymotrypsin-like activity of the proteasome, resulting in the accumulation of proteins destined for degradation by E3 ligases such as RNF180, thus functionally inhibiting RNF180. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
MLN2238 is a proteasome inhibitor that preferentially targets and inhibits the β5 subunit of the 20S proteasome. Since RNF180's function involves tagging proteins for proteasomal degradation, inhibition of the proteasome by MLN2238 would lead to the functional inhibition of RNF180 by blocking the degradation of its substrates. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib is an epoxyketone-based proteasome inhibitor. It irreversibly binds to the proteasome, inhibiting its activity. This action can inhibit the degradation pathway that RNF180 relies on for its E3 ligase activity, thus functionally inhibiting RNF180. | ||||||
Nelfinavir | 159989-64-7 | sc-507314 | 10 mg | $168.00 | ||
Nelfinavir has been shown to inhibit the proteasome indirectly. While its primary function is as an antiretroviral agent, its effect on the proteasome could disrupt the function of RNF180 by preventing the degradation of ubiquitinated proteins, which RNF180 ubiquitinates for degradation. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an oral proteasome inhibitor. By targeting the proteasomal degradation pathway, oprozomib can inhibit the function of E3 ubiquitin ligases like RNF180, leading to the accumulation of their substrates and functional inhibition of RNF180. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib is a proteasome inhibitor that covalently and selectively binds to the proteasome's active site. This binding inhibits the proteasomal degradation pathway that RNF180 uses to mediate the turnover of proteins, thereby functionally inhibiting RNF180. | ||||||