20S Proteasome β1 Activators
The chemical class 20S Proteasome β1 Activators comprises a diverse range of compounds that enhance the activity of the β1 subunit of the 20S proteasome complex, either by direct interaction or through the modulation of cellular pathways that govern the expression and functionality of the proteasome. These activators predominantly exert their effects through the upregulation of proteasome subunits via transcriptional activation pathways, such as the Nrf2-ARE pathway, which is a well-characterized mechanism for the induction of proteasome subunit expression. Compounds like Betulinic Acid, Oleanolic Acid, Curcumin, Sulforaphane, Resveratrol, and Epigallocatechin Gallate facilitate the release of Nrf2 from its inhibitor Keap1, enhancing the transcription of genes that encode the proteasome subunits, thereby augmenting the proteolytic activity of the 20S proteasome β1 subunit.
Other activators, such as Celastrol and Disulfiram, function through different mechanisms, including the induction of a heat shock response and direct binding to the proteasome, respectively. Celastrol's activation of HSF1 leads to the increased transcription of heat shock proteins and proteasome subunits, whereas Disulfiram, in the presence of copper, can directly interact with the β1 subunit to enhance its proteolytic activity. Additionally, compounds like MG132, though primarily proteasome inhibitors, are capable of transient activation of the 20S proteasome β1 subunit at sub-inhibitory concentrations. This array of molecules demonstrates the intricate regulation of proteasome activity and highlights the diverse chemical entities that activate this critical protein complex.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Betulinic Acid | 472-15-1 | sc-200132 sc-200132A | 25 mg 100 mg | $117.00 $344.00 | 3 | |
Betulinic Acid upregulates the expression of the 20S proteasome subunits by activating the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. Upon activation, Nrf2 dissociates from Keap1, translocates to the nucleus, and binds to antioxidant response elements (ARE) in the promoter regions of proteasome subunit genes, thereby increasing their transcription and 20S Proteasome β1 activity. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $53.00 $89.00 | 7 | |
Disulfiram interacts with copper to form a complex that can enter cells and bind to the 20S proteasome, resulting in its activation. This copper complex specifically interacts with the 20S proteasome β1 subunit, inducing a conformational change that increases the proteolytic activity of the proteasome. | ||||||
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 binds directly to the 20S proteasome, leading to an allosteric modification that activates its proteolytic activities. This activation is specific to the β1 subunit of the proteasome, enhancing its ability to degrade ubiquitin-independent protein substrates. | ||||||
Oleanolic Acid | 508-02-1 | sc-205775 sc-205775A | 100 mg 500 mg | $86.00 $302.00 | 8 | |
Oleanolic Acid enhances 20S proteasome activity through the induction of Nrf2. Similar to Betulinic Acid, it promotes the dissociation of Nrf2 from Keap1, leading to the expression of proteasome subunits by Nrf2-mediated transactivation. This results in increased proteasomal degradation capacity, with a specific upregulation of the β1 subunit activity. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol induces a heat shock response that results in the upregulation of 20S proteasome subunits, including the β1 subunit. By activating heat shock factor 1 (HSF1), Celastrol promotes the transcription of proteasome subunit genes, thereby enhancing the assembly and activity of the 20S proteasome complex. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Curcumin can induce the expression of proteasomal subunits through the modulation of the Keap1/Nrf2 pathway. By dissociating Nrf2 from Keap1, curcumin enhances the transcription of genes encoding the proteasome subunits, thereby facilitating the increased activity of the β1 subunit within the 20S proteasome. | ||||||
D,L-Sulforaphane | 4478-93-7 | sc-207495A sc-207495B sc-207495C sc-207495 sc-207495E sc-207495D | 5 mg 10 mg 25 mg 1 g 10 g 250 mg | $153.00 $292.00 $489.00 $1325.00 $8465.00 $933.00 | 22 | |
Sulforaphane activates the Nrf2 pathway, leading to the upregulation of proteasome subunits, including the β1 subunit of the 20S proteasome. It promotes the dissociation of Nrf2 from Keap1, enabling Nrf2 to translocate to the nucleus and bind to the ARE, thus stimulating the expression of proteasome subunit genes and enhancing 20S Proteasome β1 activity. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol has been shown to increase the proteasome activity by enhancing the transcription of its subunits through the SIRT1-mediated deacetylation of Nrf2. Deacetylated Nrf2 is more stable and has a higher DNA binding affinity, leading to increased transcription of proteasome subunit genes, including those encoding the β1 subunit, thus activating the 20S proteasome. | ||||||
t-Butylhydroquinone | 1948-33-0 | sc-202825 | 10 g | $67.00 | 4 | |
Tert-Butylhydroquinone (tBHQ) activates the Nrf2 pathway, which results in enhanced transcription of proteasome subunit genes, including the β1 subunit. tBHQ stabilizes Nrf2 by preventing its ubiquitination and degradation, thus facilitating Nrf2's nuclear translocation and subsequent activation of proteasomal gene expression, leading to an increase in 20S Proteasome β1 activity. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $43.00 $73.00 $126.00 $243.00 $530.00 $1259.00 | 11 | |
Epigallocatechin Gallate (EGCG) is known to enhance Nrf2 activity, leading to the transcription of antioxidant response genes including those encoding proteasome subunits. The enhanced expression and activity of the β1 subunit of the 20S proteasome is a consequence of the EGCG-induced Nrf2 translocation to the nucleus and binding to the ARE. | ||||||