TBX5 Inhibitors
The chemical class known as TBX5 inhibitors comprises compounds that do not directly target TBX5 but rather influence the pathways and cellular processes that TBX5 is a part of or interacts with. These compounds are typically inhibitors of signaling molecules, receptors, kinases, and other proteins that play a role in the regulation of heart development, a key biological context where TBX5 is critically involved. By targeting these signaling pathways, such as BMP, TGF-β, Wnt, and others, these inhibitors can alter the cellular milieu or the expression of genes that TBX5 controls, thereby indirectly affecting TBX5's function. For instance, inhibitors like Dorsomorphin and LDN-193189 target the BMP signaling pathway by inhibiting the BMP type I receptors. BMP signaling is crucial for cardiac development and interacts with TBX5 to regulate gene expression. Disruption of this signaling by the inhibitors can lead to changes in the transcriptional regulation of genes, affecting TBX5's role in heart and limb development. Similarly, inhibitors of the TGF-β pathway, such as SB-431542, can modulate the activity of TBX5 by influencing its transcriptional activity through altering the TGF-β signaling cascade.
Additionally, small molecule inhibitors like Y-27632 and Thiazovivin affect cellular processes such as actin cytoskeleton dynamics and cell adhesion, which are crucial for heart morphogenesis. TBX5's pivotal role during this process means that any modulation of these cellular processes can influence TBX5's expression patterns and function. Inhibition of Wnt signaling by compounds like IWP-2, IWR-1, and XAV-939 affects β-catenin levels, which are important for cardiac development and for the interaction with TBX5 in regulating gene expression. Furthermore, BIO, a GSK-3 inhibitor, can have a complex effect on TBX5's transcriptional activity by altering β-catenin stability. These inhibitors, though not directly targeting TBX5, provide valuable tools for modulating the intricate network of signaling pathways and cellular processes that TBX5 is a part of.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
BML-275 | 866405-64-3 | sc-200689 sc-200689A | 5 mg 25 mg | $94.00 $348.00 | 69 | |
BML-275 (Dorsomorphin) inhibits BMP signaling by targeting the BMP type I receptors ALK2, ALK3, and ALK6, which indirectly affects TBX5 by altering the transcriptional regulation of genes involved in cardiac development and function. BMP signaling is implicated in heart development, and TBX5 is known to interact with this pathway to regulate gene expression. | ||||||
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 1062368-24-4 | sc-476297 | 5 mg | $240.00 | ||
This compound, called LDN-193189, is a selective inhibitor of BMP type I receptors ALK2 and ALK3. By inhibiting these receptors, LDN-193189 disrupts BMP signaling, consequently affecting the cellular context in which TBX5 operates, leading to an alteration of its target gene expression related to heart and limb development. | ||||||
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 selectively inhibits ALK4, ALK5, and ALK7, which are activin and TGF-β type I receptors. As TBX5 functionally interacts with TGF-β signaling in cardiac myocytes, SB-431542 can alter the downstream effects of this pathway, thereby indirectly modulating the activity of TBX5 by influencing its transcriptional activity. | ||||||
Thiazovivin | 1226056-71-8 | sc-361380 sc-361380A | 10 mg 25 mg | $278.00 $622.00 | 15 | |
Thiazovivin is a ROCK inhibitor that can indirectly affect TBX5 by altering actin cytoskeleton dynamics and cell adhesion, processes that are crucial for proper heart morphogenesis, a developmental stage where TBX5 plays a pivotal role. Modulation of these cellular processes can influence the expression patterns and function of TBX5. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 is another potent inhibitor of ROCK. By modifying the actin cytoskeleton, cell contractility, and adhesion, Y-27632 has the potential to affect cellular processes that are essential for heart development and thus could indirectly alter TBX5's role in cardiac cell lineage specification and function. | ||||||
IWP-2 | 686770-61-6 | sc-252928 sc-252928A | 5 mg 25 mg | $94.00 $286.00 | 27 | |
IWP-2 inhibits Wnt production by inhibiting Porcupine, a membrane-bound O-acyltransferase. While TBX5 is not directly influenced by Wnt signaling, Wnt/β-catenin signaling is important in cardiac development, and TBX5 has been shown to act synergistically with Wnt signaling to regulate gene expression. | ||||||
IWR-1-endo | 1127442-82-3 | sc-295215 sc-295215A | 5 mg 10 mg | $82.00 $132.00 | 19 | |
IWR-1 is an inhibitor of the Wnt response by stabilizing the axin destruction complex, reducing β-catenin levels. As Wnt signaling can interact with TBX5 activity during cardiogenesis, IWR-1’s action can modify the cellular milieu influencing TBX5 function and its regulatory cascade in heart formation. | ||||||
XAV939 | 284028-89-3 | sc-296704 sc-296704A sc-296704B | 1 mg 5 mg 50 mg | $35.00 $115.00 $515.00 | 26 | |
XAV-939 inhibits Wnt signaling by promoting β-catenin degradation. TBX5 interacts with β-catenin in the regulation of cardiac gene expression, therefore XAV-939’s action can lead to an indirect modulation of TBX5's activity in the heart by perturbing β-catenin’s availability and its interaction with TBX5. | ||||||
GSK-3 Inhibitor IX | 667463-62-9 | sc-202634 sc-202634A sc-202634B | 1 mg 10 mg 50 mg | $57.00 $184.00 $867.00 | 10 | |
BIO (GSK-3 Inhibitor IX), which can lead to an accumulation of β-catenin by preventing its degradation. While typically associated with Wnt pathway activation, in the context of TBX5, which can interact with β-catenin, the increase in β-catenin levels may have a complex modulatory effect on TBX5-dependent transcriptional outcomes. | ||||||
Pifithrin-α hydrobromide | 63208-82-2 | sc-45050 sc-45050A | 5 mg 25 mg | $118.00 $287.00 | 36 | |
Pifithrin-α(HBr) is known as an inhibitor of p53, which interacts with several developmental pathways including those involving TBX5. By inhibiting p53, Pifithrin-α can indirectly influence TBX5’s role in the regulation of cardiac gene expression and developmental processes by modifying the p53-dependent control mechanisms in these pathways. | ||||||