Chemical inhibitors of PLAGL2 encompass a range of compounds that target the TGF-beta signaling pathway, which is pivotal for the transcriptional regulation activities of PLAGL2. SB-431542, LY364947, GW788388, SD-208, A-83-01, and LY2157299 are such inhibitors that specifically bind to TGF-beta type I receptors ALK4, ALK5, and ALK7. Their inhibition action decreases the phosphorylation of SMAD2/3, a critical step for the subsequent activation of transcription factors that interact directly with PLAGL2. In essence, these chemicals disrupt the initial signal that would normally lead to the activation of PLAGL2's transcriptional activity. Compounds like RepSox also inhibit ALK5, ensuring that the TGF-beta pathway is sufficiently suppressed to prevent the downstream effects that would culminate in PLAGL2 activity.
Further along the spectrum of PLAGL2 inhibitors are chemicals that act on intersecting signaling pathways. LDN-193189 and DMH1, for example, target ALK2 and ALK3 receptors of the bone morphogenetic protein (BMP) pathway, which has significant crosstalk with TGF-beta signaling. By inhibiting these receptors, they indirectly mitigate the influence of TGF-beta on PLAGL2, reducing its transcriptional influence. EW-7197 is also included in this group, functioning by similar mechanisms to inhibit the downstream signaling processes that would normally enhance PLAGL2's role in gene regulation. These chemicals collectively ensure that the signal transduction usually responsible for activating PLAGL2's transcriptional activity is interrupted, leading to its functional inhibition. By targeting these specific nodes within the TGF-beta and BMP pathways that interact with PLAGL2, these inhibitors are effective in reducing the regulatory influence of PLAGL2 on gene expression.
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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 | |
Inhibits the TGF-beta pathway which PLAGL2 is involved in by specifically inhibiting TGF-beta type I receptors ALK4, ALK5, and ALK7, leading to decreased SMAD2/3 phosphorylation and thus reducing PLAGL2-mediated transcriptional activation. | ||||||
LY 364947 | 396129-53-6 | sc-203122 sc-203122A | 5 mg 10 mg | $105.00 $153.00 | 4 | |
Acts as a selective inhibitor of TGF-beta type I receptor ALK5, thereby inhibiting the SMAD2/3 phosphorylation. As PLAGL2 functions downstream of the TGF-beta pathway, this inhibition would reduce PLAGL2-mediated effects. | ||||||
GW788388 | 452342-67-5 | sc-363544 sc-363544A | 5 mg 25 mg | $95.00 $384.00 | ||
A potent inhibitor of TGF-beta receptors ALK5 and ALK4, which would suppress the downstream signaling including the phosphorylation of SMAD2/3, consequently inhibiting the transcriptional activity regulated by PLAGL2. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $86.00 | 3 | |
A selective inhibitor of TGF-beta receptor 1 (ALK5), which blocks the TGF-beta/SMAD pathway, leading to a reduction in SMAD2/3-mediated transcriptional activity where PLAGL2 is involved. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $198.00 $650.00 | 16 | |
Specifically inhibits ALK5, ALK4, and ALK7, reducing SMAD2/3 activation. Since PLAGL2 functions downstream of this pathway, its signaling and consequent transcriptional activities would be inhibited. | ||||||
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 1062368-24-4 | sc-476297 | 5 mg | $240.00 | ||
Blocks ALK2 and ALK3, which are part of the BMP pathway that intersects with TGF-beta signaling, thus indirectly inhibiting PLAGL2 activity which is modulated by TGF-beta pathway inputs. | ||||||
DMH-1 | 1206711-16-1 | sc-361171 sc-361171B sc-361171A sc-361171C | 10 mg 25 mg 50 mg 100 mg | $209.00 $312.00 $620.00 $1026.00 | 2 | |
Inhibits ALK2, leading to decreased BMP signaling which indirectly affects the TGF-beta pathway and thus inhibits PLAGL2 activity that is modulated by BMP/TGF-beta pathway signaling. | ||||||
LY2157299 | 700874-72-2 | sc-391123 sc-391123A | 5 mg 10 mg | $209.00 $352.00 | 3 | |
Targets TGF-beta receptor kinase, particularly ALK5, leading to a disruption in the downstream signaling that PLAGL2 is part of, thereby inhibiting its transcriptional regulatory functions. | ||||||
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 | |
Inhibits ALK5, leading to the suppression of the TGF-beta signaling pathway, which is known to intersect with the transcriptional regulation by PLAGL2, resulting in its functional inhibition. | ||||||
EW-7197 | 1352608-82-2 | sc-507465 | 5 mg | $345.00 | ||
An ALK5 inhibitor that effectively reduces TGF-beta-induced phosphorylation of SMAD2/3, therefore inhibiting downstream transcriptional activity where PLAGL2 is involved in gene regulation. | ||||||