Date published: 2026-5-9

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Smad2 Inhibitors

The chemical class of Smad2 inhibitors represents a sophisticated array of small molecules meticulously designed to selectively target the TGF-β type I receptor, ALK5, a pivotal component in the intricate Smad2 signaling cascade. This class of inhibitors plays a crucial role in elucidating the delicate regulatory mechanisms governing cellular processes orchestrated by Smad2 within the TGF-β signaling pathway. At the core of their mechanism, Smad2 inhibitors interfere with the phosphorylation and subsequent activation of Smad2, a linchpin step in the TGF-β signaling cascade. By specifically honing in on ALK5, these inhibitors disrupt the normal progression of Smad2-mediated responses triggered by TGF-β signaling. The intricate dance between ALK5 and Smad2 is fundamental to cellular energy homeostasis, and the targeted inhibition of this interaction provides researchers with invaluable tools to dissect the molecular intricacies underlying cellular responses.

Beyond direct inhibition, the beauty of Smad2 inhibitors lies in their capacity for indirect modulation. The key to their efficacy is the precise targeting of the receptor essential for Smad2 activation in response to TGF-β signaling. This indirect approach allows researchers to finely tune Smad2-mediated cellular processes, opening a window into the regulatory intricacies of TGF-β signaling. Researchers wield these inhibitors as powerful instruments to not only comprehend the fundamental workings of Smad2 but also to manipulate cellular processes influenced by its activity. This nuanced understanding extends to a broad spectrum of physiological and pathological conditions, unraveling the implications of aberrant TGF-β signaling in various cellular contexts. In the labyrinth of cellular signaling, Smad2 inhibitors serve as guiding lights, illuminating the pathways through which cells navigate their responses to TGF-β signals.

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Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

SB 431542

301836-41-9sc-204265
sc-204265A
sc-204265B
1 mg
10 mg
25 mg
$82.00
$216.00
$416.00
48
(1)

SB-431542 is a potent and selective inhibitor of the TGF-β receptor, particularly targeting the ALK4/5/7 receptors. By inhibiting the TGF-β signaling pathway, SB-431542 indirectly modulates Smad2 activity. TGF-β receptors phosphorylate Smad2, and this compound interferes with that activation step. Through this mechanism, SB-431542 can limit Smad2-mediated transcriptional responses and downstream cellular effects regulated by the TGF-β pathway.

SIS3 hydrochloride

521984-48-5sc-253565
5 mg
$334.00
2
(1)

SIS3 is a selective inhibitor of the TGF-β type I receptor, ALK4/5/7. By specifically blocking the phosphorylation of Smad3, SIS3 indirectly affects Smad2 signaling, as Smad3 and Smad2 share common elements in the TGF-β signaling cascade. The inhibition of Smad3 phosphorylation prevents the formation of the Smad3-Smad4 complex and subsequent nuclear translocation, modulating Smad2-mediated transcriptional responses and cellular processes influenced by TGF-β signaling.

A 83-01

909910-43-6sc-203791
sc-203791A
10 mg
50 mg
$202.00
$811.00
16
(1)

A83-01 is a selective inhibitor of the TGF-β type I receptors ALK4/5/7. Similar to SB-431542, A83-01 interferes with the TGF-β signaling pathway, blocking the activation of Smad2. This inhibition occurs at the receptor level, preventing phosphorylation and subsequent nuclear translocation of Smad2. A83-01, therefore, serves as an indirect inhibitor of Smad2-mediated responses regulated by the TGF-β pathway.

ALK5 Inhibitor II

446859-33-2sc-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
$77.00
$153.00
$219.00
$663.00
$1248.00
$4382.00
$7850.00
8
(1)

RepSox is a small molecule inhibitor of the TGF-β type I receptor, ALK5. By targeting this receptor, RepSox disrupts the phosphorylation and activation of Smad2, which is downstream in the TGF-β signaling cascade. Through inhibition of Smad2 phosphorylation, RepSox modulates the nuclear translocation of Smad2 and subsequent transcriptional responses governed by the TGF-β pathway.

LY 364947

396129-53-6sc-203122
sc-203122A
5 mg
10 mg
$107.00
$156.00
4
(1)

LY364947 is a selective inhibitor of the TGF-β type I receptor, ALK5. It hinders the phosphorylation and activation of Smad2 in response to TGF-β signaling. This inhibition of Smad2 phosphorylation disrupts the downstream signaling cascade, influencing the nuclear translocation of Smad2 and its transcriptional activity. LY364947 provides a means of indirectly inhibiting Smad2-mediated cellular processes by targeting the TGF-β pathway at the receptor level.

LY2157299

700874-72-2sc-391123
sc-391123A
5 mg
10 mg
$213.00
$359.00
3
(1)

LY2157299 is a small molecule inhibitor that selectively targets the TGF-β type I receptor, ALK5. By blocking ALK5, it interferes with the phosphorylation and activation of Smad2, a key downstream mediator of TGF-β signaling. This inhibition disrupts Smad2-mediated transcriptional responses, affecting cellular processes regulated by the TGF-β pathway.

TGF-β RI Kinase Inhibitor V

627536-09-8sc-203294
2 mg
$88.00
3
(1)

SD-208 is a potent inhibitor of the TGF-β type I receptor, ALK5. Through its action on ALK5, SD-208 prevents the phosphorylation and activation of Smad2. This inhibition interferes with the downstream signaling events regulated by Smad2, affecting its nuclear translocation and transcriptional activity. SD-208 provides an indirect means of inhibiting Smad2-mediated cellular responses by targeting the TGF-β pathway at the receptor level.

GW788388

452342-67-5sc-363544
sc-363544A
5 mg
25 mg
$95.00
$384.00
(0)

GW788388 is a selective inhibitor of the TGF-β type I receptor, ALK5. By inhibiting ALK5, GW788388 disrupts the phosphorylation and activation of Smad2, a downstream mediator of TGF-β signaling. This inhibition interferes with Smad2-mediated transcriptional responses, affecting cellular processes regulated by the TGF-β pathway. GW788388 serves as an indirect modulator of Smad2 activity by specifically targeting the receptor required for its activation in response to TGF-β signaling.

ITD 1

1099644-42-4sc-507349
10 mg
$220.00
(0)

ITD-1 is a selective inhibitor of the TGF-β type I receptor, ALK5. By targeting ALK5, ITD-1 interferes with the phosphorylation and activation of Smad2 in response to TGF-β signaling. This inhibition disrupts Smad2-mediated transcriptional responses, influencing cellular processes regulated by the TGF-β pathway. ITD-1 provides an indirect means of modulating Smad2 activity by specifically targeting the receptor essential for its activation in response to TGF-β signaling.

EW-7197

1352608-82-2sc-507465
5 mg
$345.00
(0)

EW-7197 is a selective inhibitor of the TGF-β type I receptor, ALK5. By inhibiting ALK5, EW-7197 disrupts the phosphorylation and activation of Smad2 downstream in the TGF-β signaling pathway.