dsg1α Inhibitors
Chemical inhibitors of desmoglein 1 (dsg1α) operate through various mechanisms to impede its function. LY-364947, a potent inhibitor, targets the TGF-β type I receptor activin receptor-like kinase (ALK5), which is a key component in the SMAD signaling pathway, crucial for dsg1α expression and stability. Similarly, GW788388 demonstrates its effects by selectively inhibiting both ALK5 and ALK4, leading to the impairment of SMAD2/3 phosphorylation; this is essential for dsg1α's transcriptional regulation and cell surface stabilization. SB-431542 shares a comparable mode of action, selectively inhibiting ALK4, ALK5, and ALK7, which are necessary for the activation of SMAD2/3, thereby influencing dsg1α's proper functionality.
Other compounds such as SB-525334 and SD-208 specifically inhibit ALK5, with SB-525334 reducing TGF-β-mediated SMAD2/3 phosphorylation and SD-208 acting as a TGF-β receptor I kinase inhibitor. Both disruptions in TGF-β signaling result in the inhibition of dsg1α function. A-83-01, another selective inhibitor of ALK5, ALK4, and ALK7, blocks the signaling required for dsg1α localization and function. LY2157299, also known by its investigative name, Galunisertib, prevents the phosphorylation of SMAD2/3, a vital step for the stabilization and function of dsg1α. RepSox, EW-7197, and ITD-1 are additional inhibitors that target the TGF-β/SMAD pathway at different points to suppress dsg1α functionality. RepSox inhibits ALK5, EW-7197 is an ALK5 inhibitor affecting transcriptional regulation, and ITD-1 selectively inhibits the TGF-β signaling that is crucial for dsg1α's proper function. SB-505124 and IN-1130 both inhibit ALK5, decreasing SMAD activation, which in turn affects the transcription and function of dsg1α, leading to its functional inhibition.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
LY 364947 | 396129-53-6 | sc-203122 sc-203122A | 5 mg 10 mg | $107.00 $156.00 | 4 | |
This compound is a potent inhibitor of TGF-β type I receptor activin receptor-like kinase (ALK5), which is upstream of SMAD signaling. Inhibition of ALK5 by LY-364947 can prevent SMAD activation, a pathway known to be involved in the regulation of desmoglein 1 (dsg1α) expression and function in epithelial cells, leading to the functional inhibition of dsg1α. | ||||||
GW788388 | 452342-67-5 | sc-363544 sc-363544A | 5 mg 25 mg | $95.00 $384.00 | ||
GW788388 is a selective inhibitor of ALK5 and ALK4, which are part of the TGF-β signaling pathway. By inhibiting these receptors, GW788388 impairs the phosphorylation and activation of SMAD2/3, which are critical for the transcriptional regulation and stabilization of dsg1α at the cell surface, thus functionally inhibiting dsg1α. | ||||||
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 ALK4, ALK5, and ALK7, which are necessary for the activation of SMAD2/3 in the TGF-β signaling pathway. This inhibition results in decreased transcriptional events that are required for proper dsg1α function, thereby leading to its functional inhibition. | ||||||
TGF-β RI Kinase Inhibitor VIII | 356559-20-1 | sc-203295 | 2 mg | $100.00 | 2 | |
SB-525334 is an inhibitor of ALK5, and its inhibition leads to a decrease in TGF-β-mediated SMAD2/3 phosphorylation. Since TGF-β signaling can regulate the expression and stability of dsg1α, the inhibition by SB-525334 can result in the functional inhibition of dsg1α. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $88.00 | 3 | |
SD-208 is a TGF-β receptor I kinase inhibitor, which impedes the TGF-β signaling pathway. By inhibiting this kinase, SD-208 disrupts SMAD2/3 activation and subsequent transcriptional regulation of genes including those related to dsg1α function, causing functional inhibition of dsg1α. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $202.00 $811.00 | 16 | |
A-83-01 is a selective ALK5, ALK4, and ALK7 inhibitor. It blocks the TGF-β signaling necessary for the proper localization and function of dsg1α, thus leading to its functional inhibition. | ||||||
LY2157299 | 700874-72-2 | sc-391123 sc-391123A | 5 mg 10 mg | $213.00 $359.00 | 3 | |
LY2157299, also known as Galunisertib, is an inhibitor of TGF-β receptor I. It prevents the phosphorylation of SMAD2/3, which is essential for the stabilization and function of dsg1α, resulting in its functional inhibition. | ||||||
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 an inhibitor of ALK5 kinase activity, which is involved in TGF-β signaling. By inhibiting ALK5, RepSox reduces SMAD2/3 phosphorylation, which is necessary for dsg1α function, thereby functionally inhibiting dsg1α. | ||||||
EW-7197 | 1352608-82-2 | sc-507465 | 5 mg | $345.00 | ||
EW-7197 is a selective ALK5 inhibitor that disrupts the TGF-β/SMAD signaling pathway. By doing so, it impairs the transcriptional regulation and expression of dsg1α, leading to its functional inhibition. | ||||||
ITD 1 | 1099644-42-4 | sc-507349 | 10 mg | $220.00 | ||
ITD-1 is a selective TGF-β signaling inhibitor that impairs the differentiation of cells that rely on this pathway. By inhibiting the TGF-β pathway, ITD-1 disrupts the processes that contribute to the proper function of dsg1α, resulting in its functional inhibition. | ||||||