Rpn11 Activators
Rpn11 Activators are a diverse set of chemical compounds that indirectly enhance the deubiquitinating (DUB) function of Rpn11 through the modulation of proteasome activity and ubiquitin-proteasome system dynamics. Compounds like MG132, Epoxomicin, Lactacystin, and its active form Clasto-Lactacystin β-lactone, as well as Bortezomib and its analog Velcade, Carfilzomib, and Oprozomib, functionRpn11 Activators comprise a curated set of chemical compounds that, while not directly engaging with Rpn11, create a cellular environment that necessitates or enhances its deubiquitinating activity. Compounds such as MG132 and Lactacystin, along with their respective derivatives, Clasto-Lactacystin β-lactone and Velcade (another name for Bortezomib), inhibit the proteasome, leading to an accumulation of ubiquitinated proteins. This buildup increases the substrates available to Rpn11, thereby indirectly enhancing its DUB activity as it processes and removes ubiquitin moieties in preparation for proteolytic degradation. Similarly, Epoxomicin and Carfilzomib, by selectively and irreversibly inhibiting the proteasome, cause a surge in ubiquitinated substrates, which could stimulate Rpn11 to accommodate the heightened demand for deubiquitination. Betulinic acid disrupts proteasome function in a like manner, implying a potential increase in Rpn11 activity due to substrate accumulation.
Further indirect activation of Rpn11 is suggested by the action of IU1, MLN4924, and Pyr-41, which target other components of the ubiquitin-proteasome system. IU1, by inhibiting the DUB activity of UCHL5, may lead to a compensatory upsurge in Rpn11 function as the cell seeks to maintain proteostatic balance. MLN4924 inhibits the NEDD8 activating enzyme, affecting cullin-RING ubiquitin ligase activity, which could lead to altered ubiquitination dynamics and a consequent increase in Rpn11's processing activity. Pyr-41, by irreversibly inhibiting the ubiquitin-activating enzyme E1, leads to an accumulation of ubiquitinated proteins, which would also require Rpn11-mediated deubiquitination. Collectively, these chemicals, by influencing various components and checkpoints within the ubiquitin-proteasome pathway, create a cellular context that indirectly necessitates enhanced Rpn11 activity.
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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 | |
A peptide aldehyde that inhibits the proteasomal degradation pathway. While MG132 is primarily known as a proteasome inhibitor, it can indirectly enhance the functional activity of Rpn11 by increasing the substrate availability for deubiquitination, thus potentially increasing Rpn11 activity to remove ubiquitin from proteins prior to their 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 | |
A selective and irreversible proteasome inhibitor. Epoxomicin's inhibition of the proteasome's proteolytic activity can lead to the accumulation of ubiquitinated proteins, possibly enhancing Rpn11's DUB activity by increasing its interaction with these substrates. | ||||||
IU1 | 314245-33-5 | sc-361215 sc-361215A sc-361215B | 10 mg 50 mg 100 mg | $138.00 $607.00 $866.00 | 2 | |
A small molecule that specifically inhibits the DUB activity of UCHL5, which is also associated with the proteasome. Inhibition of UCHL5 by IU1 could lead to a compensatory increase in Rpn11 activity as the proteasome adjusts to maintain its function. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
A boronic acid dipeptide that reversibly inhibits the 26S proteasome. While it is a proteasome inhibitor, bortezomib could lead to increased recognition and deubiquitination of proteins by Rpn11 due to the accumulation of polyubiquitinated proteins. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $286.00 | 1 | |
An inhibitor of NEDD8 activating enzyme that leads to the reduction of neddylation of cullin proteins, affecting ubiquitin ligase activity. This could result in altered ubiquitination patterns, thereby potentially enhancing the activity of Rpn11 as it processes different ubiquitin linkages. | ||||||
Ubiquitin E1 Inhibitor, PYR-41 | 418805-02-4 | sc-358737 | 25 mg | $360.00 | 4 | |
An irreversible inhibitor of the ubiquitin activating enzyme E1. Pyr-41 may increase the functional activity of Rpn11 by causing an accumulation of ubiquitinated substrates that require processing before proteasomal degradation. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
A specific inhibitor of the proteasome's catalytic activity. Lactacystin's blocking of proteolytic degradation could indirectly increase the functional activity of Rpn11 as it attempts to deubiquitinate substrates that are stalled in the degradation pathway. | ||||||
Betulinic Acid | 472-15-1 | sc-200132 sc-200132A | 25 mg 100 mg | $117.00 $344.00 | 3 | |
A pentacyclic triterpenoid that disrupts proteasome function. It could lead to increased Rpn11 activity by causing an accumulation of ubiquitinated proteins that require deubiquitination. | ||||||