RNF214 Inhibitors
Chemical inhibitors of RNF214 can act through various mechanisms to impede its function, primarily by disrupting the ubiquitin-proteasome pathway. MG-132, Lactacystin, Epoxomicin, Bortezomib, and Carfilzomib are proteasome inhibitors that halt the degradation of ubiquitinated proteins. As the proteasome is responsible for the breakdown of these tagged molecules, its inhibition by these chemicals leads to the accumulation of proteins that are normally destined for destruction. This build-up can sequester RNF214 in non-functional complexes or overwhelm its enzymatic capacity, as it relies on the proteasome's activity for the proper turnover of its substrates. Similarly, Clasto-Lactacystin β-lactone, as a precursor of Lactacystin, shares the same mode of action, leading to the stabilization of RNF214 substrates and impeding the normal function of RNF214.
On the other hand, MLN4924 disrupts the NEDD8-activating enzyme, perturbing the neddylation process that is crucial for the functioning of the ubiquitin-proteasome system. This can indirectly affect RNF214 by interfering with substrate processing. PYR-41 targets the upstream ubiquitination process by inhibiting the ubiquitin-activating enzyme E1, resulting in reduced ubiquitination within the cell, which could decrease RNF214 activity due to a lower availability of ubiquitinated substrates. IU1 and HBX 19818 inhibit specific deubiquitinases, USP14 and USP7 respectively, which normally remove ubiquitin from proteins, potentially leading to altered ubiquitin dynamics and challenging RNF214's role in substrate recognition and ubiquitination. Lastly, Ubistatin A and NSC 632839 inhibit the binding of ubiquitin to the proteasome and multiple deubiquitinating enzymes, respectively, both leading to an increase in ubiquitinated protein levels.
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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 | |
MG-132 inhibits the proteasome, a protein complex involved in the degradation of ubiquitinated proteins. RNF214 is an E3 ubiquitin ligase; by inhibiting proteasomal degradation, MG-132 causes accumulation of ubiquitinated proteins, which can lead to functional inhibition of RNF214. | ||||||
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 blocking proteasomal activity, lactacystin leads to an accumulation of RNF214 substrates, possibly resulting in the sequestration of RNF214 in non-functional complexes. | ||||||
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. It inhibits the degradation of proteins regulated by RNF214, leading to the potential dysfunction of RNF214 due to the buildup of its substrates. | ||||||
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 may indirectly inhibit RNF214 function by preventing the turnover of ubiquitinated proteins, which could interfere with RNF214's ligase activity. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib is an epoxyketone-based proteasome inhibitor. It leads to an accumulation of polyubiquitinated proteins, potentially inhibiting RNF214 by overwhelming its enzymatic capacity through substrate accumulation. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $286.00 | 1 | |
MLN4924 inhibits the NEDD8-activating enzyme, which is essential for the neddylation process that regulates the ubiquitin-proteasome system. Inhibition of this process could indirectly inhibit RNF214 by disrupting its substrate recognition and processing. | ||||||
Ubiquitin E1 Inhibitor, PYR-41 | 418805-02-4 | sc-358737 | 25 mg | $360.00 | 4 | |
PYR-41 is a selective inhibitor of the ubiquitin-activating enzyme E1. By inhibiting upstream ubiquitination processes, PYR-41 could indirectly inhibit RNF214 by reducing the overall ubiquitination levels within the cell. | ||||||
IU1 | 314245-33-5 | sc-361215 sc-361215A sc-361215B | 10 mg 50 mg 100 mg | $138.00 $607.00 $866.00 | 2 | |
IU1 inhibits the deubiquitinase USP14, which can remove ubiquitin from proteasome-bound proteins, preventing degradation. Inhibiting USP14 increases the proteasomal workload, which could lead to functional inhibition of RNF214 by substrate accumulation. | ||||||