Smurf2 Inhibitors
The class of Smurf2 inhibitors encompasses a diverse array of chemical compounds, each strategically designed to modulate Smurf2 activity either directly or indirectly through intricate cellular pathways. Caffeic acid, a polyphenolic compound found in various plants, has emerged as a potent indirect inhibitor of Smurf2 by exerting its influence on the transforming growth factor-beta (TGF-β) signaling pathway. In contrast, compounds such as LY364947 and A83-01 take a more direct route in inhibiting Smurf2 by specifically targeting the TGF-β receptor. LY364947, a pyrazole derivative, functions by disrupting Smurf2 recruitment and subsequent ubiquitination of TGF-β receptors. This selective interference curtails Smurf2's regulatory role in the TGF-β signaling pathway, offering a targeted approach to attenuate Smurf2-mediated cellular events. A83-01, another TGF-β receptor inhibitor, operates on a similar principle, further underscoring the significance of TGF-β receptor modulation as a viable strategy for Smurf2 inhibition.
TAK-243, a direct inhibitor of NEDD8-activating enzyme (NAE), represents a distinct class of Smurf2 inhibitors that act by disrupting cullin-RING ligase (CRL) function. As Smurf2 is a substrate of CRL, TAK-243-induced inhibition of neddylation prevents Smurf2 ubiquitination, stabilizing the protein and limiting its availability for substrate ubiquitination. The Smurf2 inhibitor class further expands with compounds like NSC 23766 and Amlexanox, which indirectly attenuate Smurf2 activity by influencing the RhoA and TAK1/MAPK pathways, respectively. NSC 23766, a selective inhibitor of RhoA-specific guanine nucleotide exchange factor (GEF), disrupts RhoA activation, impacting Smurf2 stability and subcellular localization. Amlexanox, on the other hand, targets the TAK1/MAPK pathway, inhibiting TAK1 activation and subsequently modulating Smurf2 expression and stability. Closing the spectrum of Smurf2 inhibitors is MLN4924, a direct inhibitor of NEDD8-activating enzyme (NAE). Operating on a similar principle as TAK-243, MLN4924 disrupts CRL function by preventing neddylation, thereby stabilizing Smurf2 and limiting its availability for substrate ubiquitination.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Caffeic Acid | 331-39-5 | sc-200499 sc-200499A | 1 g 5 g | $31.00 $61.00 | 1 | |
Caffeic acid inhibits Smurf2 indirectly by modulating the TGF-β signaling pathway. It interferes with TGF-β receptor activation, preventing downstream Smad2/3 phosphorylation. This disruption hampers Smurf2's ubiquitin ligase activity on TGF-β receptor components, impairing ubiquitination and degradation processes. As a result, TGF-β signaling is attenuated, leading to reduced Smurf2 activity. | ||||||
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 | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin acts as an indirect inhibitor of Smurf2 by targeting the NF-κB pathway. By inhibiting NF-κB activation, curcumin suppresses the transcription of genes involved in inflammation and tumorigenesis, including Smurf2. Consequently, the reduced expression of Smurf2 limits its availability and diminishes its impact on substrates such as TGF-β receptors, impeding downstream signaling events. | ||||||
LY 364947 | 396129-53-6 | sc-203122 sc-203122A | 5 mg 10 mg | $105.00 $153.00 | 4 | |
LY364947 functions as a direct inhibitor of the TGF-β receptor, obstructing Smurf2 activation. By specifically targeting the kinase domain of TGF-β type I receptor, LY364947 interferes with Smurf2 recruitment and ubiquitination of TGF-β receptors. This disruption curtails Smurf2's ability to regulate TGF-β signaling, ultimately mitigating its impact on cellular processes influenced by Smurf2-mediated ubiquitination. | ||||||
SB 431542 | 301836-41-9 | sc-204265 sc-204265A sc-204265B | 1 mg 10 mg 25 mg | $80.00 $212.00 $408.00 | 48 | |
SB431542 inhibits Smurf2 indirectly by impeding the TGF-β/Activin/Nodal pathway. Acting as a selective TGF-β receptor inhibitor, SB431542 interferes with receptor phosphorylation and downstream Smad2/3 activation. This disruption hampers Smurf2's interaction with phosphorylated Smads, hindering its ubiquitin ligase activity. Consequently, the ubiquitination and degradation of target proteins involved in TGF-β signaling are reduced, limiting Smurf2-mediated cellular effects. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol serves as an indirect inhibitor of Smurf2 by modulating the Wnt/β-catenin pathway. By promoting GSK-3β activity, resveratrol enhances β-catenin phosphorylation and degradation. This alteration interferes with Smurf2-mediated ubiquitination of β-catenin, diminishing its impact on Wnt signaling. Consequently, resveratrol-induced modulation of the Wnt pathway indirectly attenuates Smurf2 activity, impacting cellular processes regulated by Smurf2-mediated ubiquitination. | ||||||
MLN7243 | 1450833-55-2 | sc-507338 | 5 mg | $340.00 | ||
TAK-243 acts as a direct inhibitor of NEDD8-activating enzyme (NAE), disrupting cullin-RING ligase (CRL) function. Since Smurf2 is a substrate of CRL, TAK-243 inhibits Smurf2 ubiquitination by preventing its neddylation. This interference stabilizes Smurf2 and limits its availability for substrate ubiquitination. Consequently, TAK-243-induced inhibition of CRL function directly impacts Smurf2-mediated ubiquitination processes, influencing cellular events regulated by Smurf2. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $198.00 $650.00 | 16 | |
A83-01 functions as a direct inhibitor of the TGF-β receptor, disrupting Smurf2 activation. By targeting the kinase domain of TGF-β type I receptor, A83-01 interferes with Smurf2 recruitment and ubiquitination of TGF-β receptors. This interference curtails Smurf2's ability to regulate TGF-β signaling, ultimately mitigating its impact on cellular processes influenced by Smurf2-mediated ubiquitination. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $79.00 $300.00 | 32 | |
Parthenolide inhibits Smurf2 indirectly by modulating the NF-κB pathway. By preventing IκBα phosphorylation and degradation, parthenolide impedes NF-κB activation. This modulation leads to decreased transcription of genes, including Smurf2, involved in inflammation and cell survival. Consequently, reduced Smurf2 expression limits its availability and diminishes its impact on substrates, hindering downstream cellular processes influenced by Smurf2-mediated ubiquitination. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC 23766 acts as an indirect inhibitor of Smurf2 by targeting the RhoA pathway. By inhibiting the RhoA-specific guanine nucleotide exchange factor (GEF), NSC 23766 hampers RhoA activation. This disruption influences the stability and subcellular localization of Smurf2, limiting its interaction with substrates and reducing its ubiquitin ligase activity. | ||||||
Amlexanox | 68302-57-8 | sc-217630 | 10 mg | $160.00 | 2 | |
Amlexanox serves as an indirect inhibitor of Smurf2 by targeting the TAK1/MAPK pathway. By inhibiting TAK1 activation, amlexanox disrupts downstream MAPK signaling. This interference impacts Smurf2 expression and stability, limiting its availability for substrate ubiquitination. Consequently, the modulation of the TAK1/MAPK pathway indirectly attenuates Smurf2 activity, influencing cellular processes regulated by Smurf2-mediated ubiquitination. | ||||||