Rpn11 Inhibitors
Rpn11, a subunit of the 19S regulatory particle of the 26S proteasome, plays a pivotal role in the ubiquitin-proteasome pathway. The ubiquitin-proteasome system is a key cellular machinery responsible for the degradation of misfolded or redundant proteins. Proteins targeted for degradation are first tagged with multiple ubiquitin molecules, creating a polyubiquitin chain. Rpn11's primary role is in the deubiquitination process, where it functions as a metalloprotease, cleaving the isopeptide bond between the polyubiquitin chain and the substrate protein. This deubiquitination is a prerequisite for substrate proteins to be unfolded and threaded into the core particle of the proteasome for degradation. Given the essential nature of this process for cellular proteostasis, Rpn11 is considered a crucial component of the ubiquitin-proteasome system.
Rpn11 inhibitors are chemical entities that specifically target and modulate the enzymatic activity of Rpn11. These inhibitors interact with the active site of Rpn11, often coordinating with the metal ion essential for its protease activity, leading to an obstruction in the deubiquitination process. The inhibition of Rpn11's function impedes the subsequent degradation of substrate proteins, leading to an accumulation of polyubiquitinated proteins. Given the precision of these inhibitors in targeting a specific step in the protein degradation pathway, they provide an intricate tool for researchers to dissect the biochemical and cellular consequences of interrupted proteasomal processing. By studying the effects of Rpn11 inhibitors, scientists can glean a deeper understanding of cellular protein homeostasis and the ramifications of its disruption.
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| 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 | |
Bortezomib is a dipeptide boronic acid analogue that primarily targets the 26S proteasome, inhibiting its chymotrypsin-like activity. This leads to an accumulation of undegraded proteins, inducing apoptosis in cancer cells. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $40.00 | ||
Carfilzomib is an epoxyketone that irreversibly binds to the N-terminal threonine of the 20S proteasome, inhibiting its chymotrypsin-like activity. It specifically targets malignant cells and spares normal cells. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
Ixazomib is a boronic acid analogue that, once metabolized, inhibits the chymotrypsin-like activity of the 20S proteasome. This disrupts the degradation of regulatory proteins, leading to apoptosis in cancer cells. | ||||||
Delanzomib, free base | 847499-27-8 | sc-396774 sc-396774A | 5 mg 10 mg | $160.00 $300.00 | ||
Delanzomib is a boronic acid-based inhibitor of the 20S proteasome. It primarily inhibits the chymotrypsin-like activity, leading to the accumulation of undegraded proteins and apoptosis in cancer cells. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an epoxyketone that selectively inhibits the chymotrypsin-like activity of the 20S proteasome. This disrupts protein homeostasis, causing apoptosis in malignant cells. | ||||||
ONX 0914 | 960374-59-8 | sc-477437 | 5 mg | $245.00 | ||
ONX-0914 is an epoxyketone inhibitor that selectively targets the immunoproteasome subunit LMP7. It's primarily researched in the context of autoimmune diseases but can impact protein degradation in cancer cells. | ||||||
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 reversibly inhibits the chymotrypsin-like activity of the 20S proteasome. It causes the accumulation of polyubiquitinated proteins, leading to apoptosis. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $165.00 $575.00 | 60 | |
Lactacystin is a natural product that irreversibly binds to and inhibits the 20S proteasome. This binding leads to the accumulation of ubiquitinated proteins, inducing cell cycle arrest and apoptosis. | ||||||
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 natural epoxyketone that selectively inhibits the chymotrypsin-like activity of the 20S proteasome. This leads to an accumulation of polyubiquitinated proteins, triggering apoptosis in sensitive cells. | ||||||