pan-TEAD-IN-1

Overview

pan-TEAD-IN-1 (Compound 3) is an orally active pan- TEAD inhibitor targeting the palmitoylation site of TEAD , disrupting its interaction with the coactivators YAP/TAZ , thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61 ) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC 50 of 0.36 nM and an H226 cell IC 50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC 0–∞ = 228.7 μg/mL·min, T 1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers.

Application

Products | Products > Signaling Pathways > Stem Cell/Wnt | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Stem Cells | Products > Signaling Pathways > YAP

Product Information

• Catalog No.: HY-159912
• CAS No.: 3027484-09-6
• Molecular Formula: C19H16F3NO
• Molecular Weight: 331.33
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source