Smad5 Inhibitors
The class of Smad5 inhibitors comprises a set of chemicals that intricately modulate the function of the Smad5 transcription factor by selectively targeting the TGF-β signaling pathway. These inhibitors exert their effects by precisely interfering with specific receptors and signaling cascades upstream of Smad5 activation, offering insights into strategies for regulating Smad5-dependent responses in diverse cellular contexts. One representative member of this class is SB-431542 (CAS Number: 301836-43-1), a potent and selective inhibitor of the TGF-β receptor ALK5. SB-431542 disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, altering its downstream signaling responses and providing a valuable tool for exploring the consequences of modulating TGF-β pathways on Smad5 function.
Another noteworthy member is LDN-193189 (CAS Number: 1062368-49-3), a selective inhibitor of BMP type I receptors ALK2 and ALK3. By targeting the BMP-Smad1/5/8 pathway, LDN-193189 indirectly modulates Smad5 activity. This selective interference with BMP signaling presents a specific approach for investigating the role of Smad5 in BMP-mediated processes, highlighting the intricate interplay between different branches of the TGF-β superfamily. Additionally, compounds like RepSox (CAS Number: 446859-33-2) and GW788388 (CAS Number: 852391-15-2) serve as selective inhibitors of the TGF-β type I receptor ALK5, contributing to our understanding of Smad5 modulation within the TGF-β signaling network. These inhibitors collectively offer a toolbox for researchers to explore the consequences of selectively manipulating the TGF-β/Smad5 axis, providing valuable insights into strategies involving Smad5 modulation. The specificity of these inhibitors in targeting key receptors within the TGF-β signaling cascade underscores the importance of tailoring interventions to dissect the nuanced interactions between Smad5 and its regulatory pathways.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
SB 431542 | 301836-41-9 | sc-204265 sc-204265A sc-204265B | 1 mg 10 mg 25 mg | $80.00 $212.00 $408.00 | 48 | |
SB-431542 is a potent and selective inhibitor of the TGF-β receptor, targeting the ALK5 receptor subtype. By inhibiting ALK5, SB-431542 disrupts the canonical TGF-β signaling pathway, indirectly impacting Smad5 activation. This indirect inhibition occurs upstream of Smad5, interfering with its phosphorylation and subsequent nuclear translocation, ultimately modulating Smad5-dependent transcriptional responses in various cellular contexts. | ||||||
Smad3 Inhibitor, SIS3 | 1009104-85-1 | sc-222318 | 1 mg | $252.00 | 36 | |
SIS3 specifically inhibits the activity of Smad3, a closely related member of the Smad family. As Smad5 and Smad3 share common signaling pathways, the inhibition of Smad3 by SIS3 indirectly affects Smad5-mediated responses. SIS3 acts as a selective inhibitor of the TGF-β/Smad3 axis, disrupting the delicate balance between Smad3 and Smad5 activities in cellular contexts. | ||||||
ALK5 Inhibitor II | 446859-33-2 | sc-221234 sc-221234A sc-221234B sc-221234C sc-221234D sc-221234E sc-221234F | 1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g | $75.00 $150.00 $215.00 $650.00 $1224.00 $4296.00 $7818.00 | 8 | |
RepSox is a selective inhibitor of the TGF-β type I receptor ALK5, similar to SB-431542. By targeting ALK5, RepSox disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, altering its downstream signaling responses. | ||||||
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 1062368-24-4 | sc-476297 | 5 mg | $240.00 | ||
LDN-193189 is a selective inhibitor of BMP type I receptors ALK2 and ALK3, targeting the BMP-Smad1/5/8 pathway. As Smad5 is a downstream effector of BMP signaling, the inhibition of ALK2 and ALK3 by LDN-193189 indirectly modulates Smad5 activity. | ||||||
LDN-214117 | 1627503-67-6 | sc-507451 | 5 mg | $165.00 | ||
LDN-214117 is a potent and selective inhibitor of the TGF-β type I receptor ALK5, similar to SB-431542 and RepSox. By targeting ALK5, LDN-214117 disrupts TGF-β signaling, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, altering its downstream signaling responses. | ||||||
EW-7197 | 1352608-82-2 | sc-507465 | 5 mg | $345.00 | ||
EW-7197 is a small-molecule inhibitor of TGF-β type I receptor ALK5. By targeting ALK5, EW-7197 interferes with TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This inhibition occurs upstream of Smad5 phosphorylation, influencing its downstream signaling responses. | ||||||
LY2157299 | 700874-72-2 | sc-391123 sc-391123A | 5 mg 10 mg | $209.00 $352.00 | 3 | |
LY2157299 is an oral TGF-β receptor type I (ALK5) inhibitor. By targeting ALK5, Galunisertib disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, altering its downstream signaling responses. | ||||||
GW788388 | 452342-67-5 | sc-363544 sc-363544A | 5 mg 25 mg | $95.00 $384.00 | ||
GW788388 is a selective inhibitor of the TGF-β type I receptor ALK5, similar to SB-431542, RepSox, and LDN-214117. By targeting ALK5, GW788388 disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, influencing its downstream signaling responses. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $198.00 $795.00 | 16 | |
A83-01 is a selective inhibitor of the TGF-β type I receptor ALK5. By targeting ALK5, A83-01 disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, altering its downstream signaling responses. | ||||||
ITD 1 | 1099644-42-4 | sc-507349 | 10 mg | $220.00 | ||
ITD-1 is a selective inhibitor of the TGF-β type I receptor ALK5, similar to SB-431542, RepSox, LDN-214117, and GW788388. By targeting ALK5, ITD-1 disrupts TGF-β signaling cascades, leading to indirect inhibition of Smad5 activation. This interference occurs upstream of Smad5 phosphorylation, influencing its downstream signaling responses. | ||||||