RNF113A1 Inhibitors
Chemical inhibitors of RNF113A1 utilize various mechanisms to indirectly impede its E3 ubiquitin-protein ligase activity. Clasto-Lactacystin beta-lactone, Bortezomib, MG132, Epoxomicin, Lactacystin, Carfilzomib, and Oprozomib are all proteasome inhibitors that can lead to the accumulation of proteins that RNF113A1 typically marks for degradation. By binding irreversibly to the proteasomal 20S subunit, Clasto-Lactacystin beta-lactone prevents the breakdown of these proteins. Similarly, Bortezomib, a known proteasome inhibitor, impedes the breakdown of ubiquitinated proteins that RNF113A1 targets, leading to substrate overload. MG132 and Lactacystin specifically block the degradation of polyubiquitinated proteins, while Epoxomicin selectively targets the proteasome to achieve the same effect. Carfilzomib, offering a similar proteasome inhibition, ensures a buildup of RNF113A1 substrates, while Oprozomib, an orally bioavailable proteasome inhibitor, also contributes to the accumulation of these substrates.
MLN4924, on the other hand, inhibits the NEDD8-activating enzyme, which is necessary for the neddylation process that regulates SCF-type E3 ubiquitin ligases. Although RNF113A1 is not a cullin-based E3 ligase, the overall ubiquitin-proteasome system, where RNF113A1 operates, is impacted by the inhibition of this pathway. PYR-41 targets the ubiquitin-activating enzyme E1, leading to a decrease in ubiquitin conjugation, which limits the ability of RNF113A1 to modify its substrates. IU1 and HBX 41,108 work by inhibiting deubiquitinating enzymes; IU1 targets USP14, which can change the rate of degradation of ubiquitinated proteins, while HBX 41,108 targets USP7, affecting the turnover of ubiquitin-protein conjugates, thereby influencing the ubiquitination equilibrium and indirectly affecting RNF113A1's ligase activity. These inhibitors collectively demonstrate the intricate relationship between proteasome function, ubiquitin conjugation, and deubiquitination processes that govern RNF113A1's role in protein regulation.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $165.00 $575.00 | 60 | |
Lactacystin specifically inhibits the proteasome, which would lead to an accumulation of RNF113A1 substrates and could indirectly inhibit the function of RNF113A1 by reducing the efficiency of substrate ubiquitination due to feedback mechanisms. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $280.00 | 1 | |
MLN4924 inhibits the NEDD8-activating enzyme, which is essential for the neddylation of cullin proteins that regulate SCF-type E3 ubiquitin ligases. Although RNF113A1 is not a cullin-based E3 ligase, the neddylation pathway influences the ubiquitin-proteasome system, where RNF113A1 functions, indirectly inhibiting its activity. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $132.00 $1064.00 | 115 | |
Bortezomib is a proteasome inhibitor that impedes the breakdown of ubiquitinated proteins, thereby potentially causing an accumulation of RNF113A1 substrates and indirect inhibition of RNF113A1's ligase activity due to substrate overload and feedback inhibition. | ||||||
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 | |
As a proteasome inhibitor, MG132 blocks the degradation of polyubiquitinated proteins, indirectly impacting RNF113A1 function by preventing the recycling of ubiquitin and degradation of its substrates, which is essential for the sustained activity of ubiquitin-protein ligases. | ||||||
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 | |
This chemical is a selective proteasome inhibitor that impedes the degradation pathway crucial for E3 ubiquitin ligases like RNF113A1, leading to an indirect inhibition by feedback due to accumulation of ubiquitinated proteins. | ||||||
Ubiquitin E1 Inhibitor, PYR-41 | 418805-02-4 | sc-358737 | 25 mg | $360.00 | 4 | |
PYR-41 is an inhibitor of ubiquitin-activating enzyme E1, a key enzyme in the ubiquitin-proteasome pathway where RNF113A1 functions. By inhibiting E1, PYR-41 would lead to a decrease in ubiquitin conjugation, indirectly inhibiting RNF113A1 activity by limiting its substrate modification potential. | ||||||
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 deubiquitinating enzyme USP14, which can regulate the degradation of ubiquitinated proteins by the proteasome. The inhibition of USP14 can result in enhanced degradation of proteins, potentially counteracting the activity of RNF113A1 by depleting its substrates more rapidly. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $40.00 | ||
Carfilzomib is a selective proteasome inhibitor that would lead to an accumulation of substrates for RNF113A1, potentially causing feedback inhibition of the E3 ligase activity due to the saturation of the ubiquitin-proteasome system. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an orally bioavailable proteasome inhibitor. By inhibiting the proteasome, oprozomib would result in an accumulation of RNF113A1's substrates, leading to an indirect inhibition of RNF113A1's E3 ubiquitin ligase activity due to substrate backlog. | ||||||