tead 3

YAP-TEAD-IN-3 is an inhibitor of YAP/TAZ-TEAD interactions with an IC50 of 9 nM for Avi-human TEAD (4217-434). YAP-TEAD-IN-3 inhibits YAP reporter gene expression (IC50 = 0.048 μM) and NCI-H2052 cell proliferation (IC50 = 0.048 μM).

TEAD-IN-3 (compound I-177) is a potent inhibitor of the TEAD transcription factor, which can be used to study proliferative diseases such as cancer.

pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP/TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC50 of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg/mL·min, T1/2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.

TEAD1/3/4-IN-1 (compound 1) is an inhibitor of TEAD1/3/4 that suppresses YAP/TAZ-TEAD interactions. It exhibits antitumour activity against NF2-deficient NCI-H226 cells and may be employed in studies of cancer and diseases mediated by Hippo pathway abnormalities.

MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.

YAP/TAZ inhibitor-2 is a potent, orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM, demonstrating anti-proliferative and antitumor activity [1].

MYF-03-176 is an orally active TEAD1/3/4 inhibitor with IC₅₀ values of 47/32/71 nM, respectively. It also inhibits TEAD transcriptional activity and cell growth in NCI-H226 cells, exhibiting antitumour activity in malignant pleural mesothelioma (MPM) cells with defective Hippo signalling and in mouse xenograft models.