PTGF-β Inhibitors
Chemical inhibitors of PTGF-β operate through various mechanisms to impede the signaling pathways that are vital for its function. SB-431542, LY2109761, Galunisertib, and RepSox are all inhibitors that target the activin receptor-like kinase (ALK) receptors, which are pivotal components of the TGF-β signaling pathway. By inhibiting the kinase activity of ALK4, ALK5, and ALK7, these chemicals prevent the phosphorylation of Smad2/3, a crucial step in PTGF-β signal transduction. For example, Galunisertib blocks the phosphorylation and activation of Smad2/3 proteins by inhibiting ALK5 kinase activity, directly reducing the functional activity of PTGF-β signaling. Similarly, RepSox targets the ALK5 kinase domain, leading to an obstacle in the TGF-β/Smad pathway and thereby inhibiting PTGF-β's activity.
Further down the PTGF-β signaling pathway, chemicals like Pirfenidone and Tranilast work by attenuating TGF-β signaling, but through a different mechanism. These inhibitors act by obstructing the downstream phosphorylation of Smad2/3, which is essential for the transmission of PTGF-β mediated signals. Tranilast, specifically, disrupts the nuclear translocation of Smad2/3, resulting in a blockade of PTGF-β's effects within the cell. Other inhibitors, such as LY364947 and GW788388, also effectively inhibit ALK5 kinase activity, with GW788388 extending its inhibition to ALK4. This dual inhibition by GW788388 strongly impairs TGF-β-induced phosphorylation of Smad2/3, culminating in a substantial functional inhibition of PTGF-β. SD-208, A83-01, and Vactosertib also selectively inhibit ALK5, ALK4, and ALK7 to varying extents, which translates into suppression of TGF-β/Smad signaling and the functional inhibition of PTGF-β.
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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 | $82.00 $216.00 $416.00 | 48 | |
SB-431542 selectively inhibits the activin receptor-like kinase (ALK) receptors which are part of the TGF-β signaling pathway. By inhibiting ALK4, ALK5, and ALK7, this chemical prevents the phosphorylation of Smad2/3, thus functionally inhibiting PTGF-β's signal transduction. | ||||||
LY2109761 | 700874-71-1 | sc-396262 sc-396262A | 1 mg 5 mg | $89.00 $275.00 | 9 | |
LY2109761 is a selective inhibitor of TGF-β receptor type I (ALK5) and type II (TGFβRII), which impedes the kinase activity of these receptors, thereby functionally inhibiting PTGF-β signaling by preventing Smad2/3 activation. | ||||||
LY2157299 | 700874-72-2 | sc-391123 sc-391123A | 5 mg 10 mg | $213.00 $359.00 | 3 | |
LY2157299 inhibits ALK5, a TGF-β receptor kinase, thus blocking the phosphorylation and activation of Smad2/3 proteins and functionally inhibiting PTGF-β signaling. | ||||||
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 | $77.00 $153.00 $219.00 $663.00 $1248.00 $4382.00 $7850.00 | 8 | |
RepSox is a small molecule inhibitor that targets the ALK5 kinase domain, leading to inhibition of the TGF-β/Smad signaling pathway and functional inhibition of PTGF-β activity. | ||||||
Pirfenidone | 53179-13-8 | sc-203663 sc-203663A | 10 mg 50 mg | $102.00 $416.00 | 6 | |
Pirfenidone can attenuate TGF-β signaling through inhibition of the downstream Smad2/3 phosphorylation, thus functionally inhibiting PTGF-β mediated cellular responses. | ||||||
Tranilast | 53902-12-8 | sc-200389 sc-200389A sc-200389B sc-200389C | 10 mg 50 mg 1 g 5 g | $31.00 $103.00 $283.00 $978.00 | 2 | |
Tranilast interferes with TGF-β signaling by inhibiting Smad2/3 phosphorylation and nuclear translocation, resulting in functional inhibition of PTGF-β. | ||||||
LY 364947 | 396129-53-6 | sc-203122 sc-203122A | 5 mg 10 mg | $107.00 $156.00 | 4 | |
LY364947 is a potent inhibitor of ALK5 kinase activity, leading to the blockade of TGF-β signaling and subsequent functional inhibition of PTGF-β. | ||||||
GW788388 | 452342-67-5 | sc-363544 sc-363544A | 5 mg 25 mg | $95.00 $384.00 | ||
GW788388 is a potent inhibitor of both ALK5 and ALK4, impairing TGF-β-induced phosphorylation of Smad2/3 and functionally inhibiting the PTGF-β signaling cascade. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $88.00 | 3 | |
SD-208 is a TGF-βRI kinase inhibitor that prevents TGF-β signaling, resulting in functional inhibition of PTGF-β by blocking the phosphorylation and nuclear translocation of Smad proteins. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $202.00 $811.00 | 16 | |
A83-01 selectively inhibits ALK5, ALK4, and ALK7, disrupting the TGF-β signaling pathway and leading to functional inhibition of PTGF-β. | ||||||