YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM).
CAT No: R1804
CAS No:1659305-78-8
Synonyms/Alias:YAP-TEAD Inhibitor 1;CHEMBL3335461;1659305-78-8;EX-A7824;BDBM50497300;NSC837892;AKOS032945175;CCG-270697;NSC-837892;
YAP-TEAD Inhibitor 1 is a small molecule compound designed to disrupt the interaction between Yes-associated protein (YAP) and TEA domain family transcription factors (TEADs), a pivotal signaling axis within the Hippo pathway. As a potent modulator of transcriptional co-activation, it has emerged as a valuable research tool for investigating the molecular mechanisms underlying cell proliferation, organ size regulation, and tissue homeostasis. The compound's ability to selectively interfere with YAP-TEAD complex formation renders it highly relevant for studies focused on transcriptional regulation, signaling pathway elucidation, and target validation in diverse biological systems.
Pathway Analysis: Researchers utilize YAP-TEAD Inhibitor 1 in the functional dissection of the Hippo signaling pathway, which governs key processes such as cell growth, apoptosis, and stem cell maintenance. By specifically blocking YAP-TEAD interactions, the inhibitor enables precise interrogation of downstream gene expression profiles, facilitating the identification of Hippo pathway target genes and regulatory feedback loops. This targeted approach allows scientists to delineate the contribution of YAP-TEAD signaling to cellular phenotypes and to unravel pathway crosstalk with other growth regulatory networks.
Transcriptional Regulation Studies: The compound serves as an essential tool for probing the transcriptional machinery associated with YAP and TEAD. By preventing the assembly of the YAP-TEAD transcriptional complex, it provides a means to assess the direct impact of this interaction on gene expression dynamics. Researchers can employ it in reporter assays, chromatin immunoprecipitation experiments, and transcriptomic analyses to quantify changes in transcriptional activity upon disruption of YAP-TEAD binding, thereby advancing the understanding of gene regulatory mechanisms in development and disease models.
Cell Proliferation and Differentiation Research: YAP-TEAD Inhibitor 1 is widely applied in studies investigating the molecular determinants of cell proliferation, differentiation, and fate specification. Its use enables the assessment of how YAP-TEAD-dependent transcription influences cell cycle progression, stemness, and lineage commitment in various cell types. By modulating this signaling node, researchers can dissect the role of Hippo pathway effectors in the maintenance of tissue architecture and the regulation of regenerative processes, making the compound highly valuable for developmental biology and stem cell research.
Target Validation and Drug Discovery: In the context of early-stage drug discovery, the inhibitor is frequently employed to validate YAP-TEAD as a molecular target in diverse cellular models. Its selective disruption of protein-protein interactions allows for the assessment of downstream phenotypic consequences, facilitating the identification of potential therapeutic targets and biomarkers. High-content screening and mechanistic studies leveraging this compound contribute to the prioritization of novel modulators of the Hippo pathway, supporting the rational design of future chemical probes and candidate molecules.
Mechanistic Elucidation of Protein-Protein Interactions: The compound is instrumental in studies focused on the structural and functional characterization of protein-protein interactions within the Hippo pathway. By serving as a chemical probe, it aids in mapping the interaction interfaces between YAP and TEAD, supporting efforts in structural biology, computational modeling, and mutagenesis analyses. This mechanistic insight is crucial for advancing the design of next-generation inhibitors and for understanding the broader principles governing transcriptional co-activator complexes in eukaryotic cells.
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