Smurf2 Activators
Smurf2, a crucial E3 ubiquitin ligase, is subject to modulation by a diverse array of compounds identified as Smurf2 activators. Within this chemical class, Nordihydroguaiaretic Acid (NDGA) emerges as a notable member. NDGA disrupts the Smurf2-Smad7 complex, freeing Smurf2 to ubiquitinate and degrade key components in the TGF-β signaling cascade. This targeted disruption underscores the specificity of NDGA in unleashing Smurf2 activity within the context of TGF-β signaling. Another distinctive member, Withaferin A, interacts with Hsp90 to destabilize the Hsp90-Smurf2 complex, resulting in enhanced Smurf2 ubiquitin ligase activity. This interaction proves critical in promoting the targeted degradation of specific substrates implicated in TGF-β signaling pathways, providing a unique mode of Smurf2 activation within cellular contexts. MRT68921 represents another intriguing compound within this class, indirectly activating Smurf2 by inhibiting ULK1. This inhibition disrupts autophagy-mediated degradation of Smurf2, leading to increased ubiquitin ligase activity against TGF-β signaling components. This indirect mechanism sheds light on the complex regulatory networks influencing Smurf2 activation.
The chemical class further encompasses compounds like TAK-632 and GSK'963, which exert their influence on Smurf2 indirectly by targeting distinct cellular pathways. TAK-632, through MEK inhibition, alters the expression of SPRY4, ultimately enhancing Smurf2 activation. On the other hand, GSK'963 disrupts the negative regulation of Smurf2 by the NF-κB pathway, resulting in increased Smurf2 activity. The multifaceted nature of these compounds emphasizes the intricate interplay of cellular pathways in modulating Smurf2 function, offering a nuanced understanding of the chemical landscape governing Smurf2 activation. In conclusion, the Smurf2 activators exhibit diverse mechanisms of action, reflecting the complexity of Smurf2 regulation. These compounds serve as invaluable tools for dissecting the intricate pathways and molecular interactions that govern Smurf2 activity, contributing to a comprehensive understanding of its role in cellular processes, particularly within the TGF-β signaling cascade.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
NDGA (Nordihydroguaiaretic acid) | 500-38-9 | sc-200487 sc-200487A sc-200487B | 1 g 5 g 25 g | $109.00 $384.00 $2190.00 | 3 | |
NDGA inhibits the ubiquitin ligase activity of Smurf2 by disrupting the formation of the Smurf2-Smad7 complex. This disrupts the negative feedback loop on TGF-β signaling, leading to enhanced Smurf2 activation and subsequent ubiquitination. | ||||||
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 modulates Smurf2 activity by interacting with Hsp90 and disrupting the Hsp90-Smurf2 complex. This leads to increased Smurf2 ubiquitin ligase activity, promoting the degradation of specific substrates involved in TGF-β signaling pathways. | ||||||
MRT 68921 | 1190379-70-4 | sc-507429 | 10 mg | $276.00 | ||
MRT68921 is a potent inhibitor of ULK1, a kinase involved in autophagy. Inhibiting ULK1 disrupts the autophagy-mediated degradation of Smurf2, leading to its accumulation and increased ubiquitin ligase activity against TGF-β signaling components. | ||||||
CCT036477 | 305372-78-5 | sc-391631A sc-391631 | 5 mg 25 mg | $109.00 $437.00 | 1 | |
CCT036477 inhibits PAK4, a kinase implicated in cell migration. By suppressing PAK4 activity, it indirectly activates Smurf2, as PAK4 is known to phosphorylate and inhibit Smurf2. This inhibition relieves the suppression on TGF-β signaling, enhancing Smurf2 function. | ||||||
(S)-HDAC-42 | 935881-37-1 | sc-296364 sc-296364A | 1 mg 5 mg | $96.00 $417.00 | ||
AR-42 is a HDAC inhibitor that alters the acetylation status of Smurf2. This modification enhances the stability and activity of Smurf2, leading to increased ubiquitination of TGF-β receptor-associated Smads and consequent potentiation of Smurf2's pro-degradative function. | ||||||
TAK 632 | 1228591-30-7 | sc-473801 | 5 mg | $228.00 | ||
TAK-632 is a MEK inhibitor that indirectly influences Smurf2. By suppressing the MAPK pathway through MEK inhibition, it alters the expression of SPRY4, a negative regulator of the TGF-β pathway, leading to increased Smurf2 activation and enhanced degradation of target proteins. | ||||||
CCT241533 | 1262849-73-9 | sc-507308 | 10 mg | $440.00 | ||
CCT241533 inhibits the phosphorylation of EIF4E by MNK1/2, modulating translation initiation. This indirectly activates Smurf2 by preventing the translation of Smurf2-specific mRNAs, leading to reduced Smurf2 levels and enhanced stability of TGF-β signaling components. | ||||||
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $265.00 $944.00 | 5 | |
C646 is a selective inhibitor of p300/CBP HAT, impacting the acetylation status of Smurf2. By altering the acetylation profile, it enhances the stability and activity of Smurf2, leading to increased ubiquitination and degradation of TGF-β receptor-associated Smads. | ||||||
A66 | 1166227-08-2 | sc-364394 sc-364394A | 5 mg 50 mg | $255.00 $1455.00 | ||
A66 inhibits the activity of AKT, a kinase involved in cell survival pathways. By suppressing AKT, it indirectly activates Smurf2, as AKT is known to phosphorylate and inhibit Smurf2. This inhibition relieves the suppression on TGF-β signaling, enhancing Smurf2 function. | ||||||
PRT4165 | 31083-55-3 | sc-507487 | 10 mg | $134.00 | ||
PRT4165 is a selective inhibitor of the E3 ligase HDM2, preventing the ubiquitination and degradation of Smurf2. By stabilizing Smurf2, it enhances its ubiquitin ligase activity, leading to increased degradation of TGF-β receptor-associated Smads and other pathway components. | ||||||