YAP Inhibitors
The class of YAP inhibitors comprises a diverse array of small molecules designed to modulate the activity of YAP, a key transcriptional co-activator involved in tissue growth and regeneration. These inhibitors can be broadly categorized into those that directly disrupt the YAP-TEAD interaction and those that act indirectly by targeting upstream signaling pathways. Direct inhibitors such as Combrestatin A4, CA1, SJFα, and WZ4003 specifically target the interaction between YAP and TEAD, preventing the formation of the YAP-TEAD complex. This disruption hinders YAP's transcriptional activity, impeding its ability to regulate gene expression associated with cell proliferation and survival. These inhibitors showcase a targeted approach to modulating YAP by directly interfering with its essential interactions within the Hippo signaling pathway.
Indirect inhibitors like Verteporfin, XMU-MP-1, PF-3644022, GSK-3 Inhibitor (BIO), NU6140, Kenpaullone, and XMU-MP-2 operate through different mechanisms, primarily focusing on the regulation of upstream signaling pathways. For instance, Verteporfin disrupts the Hippo pathway, while GSK-3 inhibitors stabilize β-catenin, influencing YAP through the Wnt/β-catenin pathway. XMU-MP-1 and XMU-MP-2 activate Lats1/2, promoting YAP phosphorylation and degradation. These indirect inhibitors offer a broader perspective on YAP modulation, affecting its activity through diverse cellular pathways. Overall, the chemical class of YAP inhibitors provides a versatile toolkit for researchers aiming to decipher the intricate regulatory mechanisms governing YAP-mediated cellular processes. The direct and indirect modulation strategies offer researchers nuanced approaches to studying YAP's role in tissue growth and regeneration.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Verteporfin | 129497-78-5 | sc-475698 sc-475698A | 10 mg 100 mg | $354.00 $2764.00 | 5 | |
Verteporfin is a small molecule inhibitor that indirectly targets YAP by disrupting the Hippo signaling pathway. It inhibits the interaction between YAP and TEAD, preventing YAP's nuclear translocation and transcriptional activity. This disruption hinders YAP-mediated gene expression involved in cell proliferation and survival, making Verteporfin a potential indirect inhibitor of YAP. | ||||||
Combrestatin A4 | 117048-59-6 | sc-204697 sc-204697A | 1 mg 5 mg | $46.00 $81.00 | ||
CA4 is a YAP-TEAD interaction inhibitor that disrupts the formation of the YAP-TEAD complex, hindering YAP's transcriptional activity. Through interference with YAP-TEAD interactions, CA4 modulates downstream signaling pathways, potentially inhibiting YAP-mediated cellular processes involved in tissue growth and regeneration. This compound highlights a strategy for targeting YAP indirectly by disrupting its critical interactions within the Hippo signaling pathway. | ||||||
PF-3644022 | 1276121-88-0 | sc-478487 sc-478487A | 5 mg 25 mg | $367.00 $2856.00 | ||
PF-3644022 is a selective inhibitor of the Hippo pathway, acting upstream of YAP. It activates Lats1/2, leading to YAP phosphorylation and subsequent degradation. By promoting YAP's inhibitory phosphorylation, PF-3644022 indirectly inhibits YAP's nuclear translocation and transcriptional activity. This compound provides a means to modulate YAP indirectly by regulating upstream components of the Hippo signaling pathway. | ||||||
GSK-3 Inhibitor IX | 667463-62-9 | sc-202634 sc-202634A sc-202634B | 1 mg 10 mg 50 mg | $58.00 $188.00 $884.00 | 10 | |
GSK-3 Inhibitor (BIO) is a small molecule that indirectly modulates YAP activity by targeting the Wnt/β-catenin pathway. By inhibiting GSK-3, BIO stabilizes β-catenin, which interacts with YAP, leading to its cytoplasmic sequestration and degradation. This indirect modulation disrupts YAP's nuclear translocation and transcriptional activity, providing a strategy for regulating YAP through the Wnt/β-catenin signaling axis. | ||||||
WZ4003 | 1214265-58-3 | sc-473979 | 5 mg | $300.00 | ||
WZ4003 is a YAP-TEAD interaction inhibitor that disrupts the formation of the YAP-TEAD complex, preventing YAP's transcriptional activity. By targeting the interaction interface between YAP and TEAD, WZ4003 interferes with downstream signaling events regulated by YAP, offering a potential avenue for inhibiting YAP-mediated cellular processes related to tissue growth and regeneration. | ||||||
NU 6140 | 444723-13-1 | sc-202531 | 5 mg | $147.00 | 1 | |
NU6140 is a CDK inhibitor that indirectly modulates YAP activity by regulating the cell cycle. By inhibiting CDKs, NU6140 arrests the cell cycle progression and affects YAP's nuclear translocation and transcriptional activity. This indirect modulation provides a means to influence YAP through cell cycle regulation, offering insights into the crosstalk between YAP and cell cycle progression and its implications for cellular processes related to tissue growth and regeneration. | ||||||
Kenpaullone | 142273-20-9 | sc-200643 sc-200643A sc-200643B sc-200643C | 1 mg 5 mg 10 mg 25 mg | $61.00 $153.00 $231.00 $505.00 | 1 | |
Kenpaullone is a GSK-3 inhibitor that indirectly influences YAP through the Wnt/β-catenin pathway. By inhibiting GSK-3, Kenpaullone stabilizes β-catenin, which interacts with YAP, leading to its cytoplasmic sequestration and degradation. This indirect modulation disrupts YAP's nuclear translocation and transcriptional activity, providing a strategy for regulating YAP through the Wnt/β-catenin signaling axis and influencing cellular processes related to tissue growth and regeneration. | ||||||