RNF219 Inhibitors
Chemical inhibitors of RNF219 include a variety of compounds that target the ubiquitin-proteasome pathway, where RNF219 plays a pivotal role as an E3 ubiquitin-protein ligase. Compounds such as MG-132, lactacystin, epoxomicin, bortezomib, carfilzomib, and oprozomib are proteasome inhibitors which prevent the degradation of ubiquitinated proteins. The action of these inhibitors leads to an accumulation of the proteins tagged for degradation by RNF219, which in turn functionally inhibits the protein's role in regulating proteolysis. For instance, MG-132 is a peptide aldehyde that reversibly and potently inhibits the proteasome, while lactacystin, an irreversible inhibitor, binds to the proteasome and disrupts its function. Epoxomicin, with its selective and irreversible binding to the proteasome, impedes the breakdown process that RNF219 facilitates. Bortezomib, a boronic acid dipeptide, selectively inhibits the 26S proteasome, and carfilzomib, an epoxyketone-based inhibitor, forms an irreversible bond with the proteasome, both leading to the inhibition of RNF219's function in protein catabolism.
Additional chemicals such as delanzomib, marizomib, and withaferin A also inhibit the proteasome, further contributing to the inhibition of RNF219 by preventing the degradation of its ubiquitinated substrates. Delanzomib, a boronate proteasome inhibitor, and marizomib, a natural product that binds irreversibly to the proteasome, both prevent the proteolytic breakdown of proteins that RNF219 has marked for degradation. Withaferin A, as a steroidal lactone, disrupts proteasomal activity, which is crucial for the degradation pathway that RNF219 is involved in. Auranofin, through its inhibition of thioredoxin reductase, indirectly impairs the ligase activity of RNF219 by modifying the redox environment in which RNF219 operates. MLN2238, or Ixazomib, is a reversible proteasome inhibitor that, by preventing the breakdown of ubiquitinated proteins, inhibits the ligase activity of RNF219.
SEE ALSO...
| 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 is a peptide aldehyde which acts as a potent, reversible, and cell-permeable proteasome inhibitor. RNF219 functions as an E3 ubiquitin-protein ligase, and MG-132 inhibits the proteasome's ability to degrade ubiquitinated proteins, thereby functionally inhibiting the degradation process RNF219 is involved in. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
Lactacystin is a naturally occurring compound that irreversibly inhibits proteasome activity. By inhibiting the proteasome, lactacystin leads to an accumulation of proteins ubiquitinated by E3 ligases such as RNF219, which inhibits RNF219's ability to regulate protein degradation. | ||||||
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 specifically targets the proteasome's active sites, which results in the inhibition of the degradation of proteins ubiquitinated by RNF219, thus functionally inhibiting RNF219's role in protein turnover. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib is a boronic acid dipeptide and a selective inhibitor of the 26S proteasome. By inhibiting the proteasome, Bortezomib prevents the breakdown of RNF219-ubiquitinated proteins, thereby inhibiting the functional role of RNF219 in proteasomal degradation pathways. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib is an epoxyketone-based proteasome inhibitor. It irreversibly binds to the proteasome, preventing the degradation of ubiquitinated proteins, thus inhibiting the function of RNF219 in the proteasomal degradation process. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an oral proteasome inhibitor that, by hindering the proteasome's activity, prevents the degradation of proteins ubiquitinated by RNF219, thereby functionally inhibiting RNF219's role 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 boronate proteasome inhibitor. Its inhibition of the proteasome leads to an increase in ubiquitinated proteins, which in turn inhibits the function of RNF219 by preventing the targeted degradation of its substrates. | ||||||
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 known to inhibit proteasomal activity. This inhibition leads to the accumulation of ubiquitinated proteins, which functionally inhibits the activity of RNF219 in the ubiquitin-proteasome degradation pathway. | ||||||
Auranofin | 34031-32-8 | sc-202476 sc-202476A sc-202476B | 25 mg 100 mg 2 g | $153.00 $214.00 $4000.00 | 39 | |
Auranofin is a gold-containing compound that inhibits the enzyme thioredoxin reductase. By altering the cellular redox state, it can indirectly inhibit the function of RNF219 by affecting its ligase activity, which is sensitive to redox changes. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
MLN2238, also known as Ixazomib, is a proteasome inhibitor. By selectively and reversibly inhibiting the 20S proteasome, MLN2238 causes an accumulation of ubiquitinated proteins, thus functionally inhibiting the E3 ubiquitin ligase activity of RNF219. | ||||||