| S8554 |
Super-TDU
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Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.
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Matrix Biol, 2024, S0945-053X(24)00107-0
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Gut Microbes, 2023, 15(1):2192501
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Cell Death Discov, 2023, 9(1):424
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| S8951 |
TED-347
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TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. This compound inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM.
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Viruses, 2025, 17(3)400
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Aging Cell, 2023, e13913.
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Sci Adv, 2023, 9(28):eadf9460
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| E1490 |
IAG933
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IAG933 (YAP-TEAD-IN-3) is a small molecule and acts as a YAP/TAZ-TEAD inhibitor. It also inhibits NCI-H2052 and can be used in research of tumor invasion and metastatic spread of solid tumors.
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FEBS Open Bio, 2024, 10.1002/2211-5463.13901
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| E1976 |
BAY-593
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BAY-593 is an in vivo probe and small molecule inhibitor of geranylgeranyltransferase-I (GGTase-I), blocking oncogenic YAP1/TAZ. It exhibits potent anti-tumor activity and inhibits cancer cell proliferation in vitro.
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| E1563 |
GNE-7883
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GNE-7883 is a potent and allosteric small-molecule inhibitor of pan-TEAD, that allosterically blocks the interactions between YAP/TAZ and all human TEAD paralogs through binding to the TEAD lipid pocket. It effectively reduces chromatin accessibility at TEAD motifs, suppresses cell proliferation in a variety of cell line models and achieves strong antitumor efficacy in vivo. Furthermore, it effectively overcomes KRAS G12C inhibitor resistance.
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| S1786 |
Verteporfin
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Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
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Nat Commun, 2025, 16(1):4124
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Adv Sci (Weinh), 2025, 12(44):e11726
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Cell Death Differ, 2025, 10.1038/s41418-025-01446-2
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| S8661 |
CA3 (CIL56)
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CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).
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Gastric Cancer, 2025, 10.1007/s10120-025-01630-w
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Viruses, 2025, 17(3)400
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Sci Rep, 2025, 15(1):26968
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| S8164 |
YAP-TEAD Inhibitor 1 (Peptide 17)
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YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM.
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Adv Sci (Weinh), 2025, 12(36):e09361
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EMBO Mol Med, 2025, 10.1038/s44321-025-00278-4
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Stem Cell Res Ther, 2025, 16(1):489
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| S8184 |
Cytochalasin D
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Cytochalasin D (Zygosporin A, NSC 209835) is a potent actin polymerization inhibitor derived from fungus. Cytochalasin D inhibits actin filament dynamics in cells. It induces phosphorylation and cytoplasmic retention of Yap.
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Nat Commun, 2025, 16(1):4069
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Cell Regen, 2025, 14(1):21
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Cell Prolif, 2024, e13728.
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| E1061 |
TRULI (Lats-IN-1)
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TRULI inhibits both Lats1 and Lats2 with a IC50 of 0.2 nM, suppresses Yap phosphorylation, induces cell proliferation in several cell lines and tissues, and promotes the initial stages of proliferative regeneration of the sensory receptors in the inner ear.
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Cell, 2025, S0092-8674(25)00807-4
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Nat Commun, 2024, 15(1):5449
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Cell Rep, 2024, 43(4):114032
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| E1314 |
TDI-011536
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TDI-011536 is a potent Lats kinase inhibitor that interrupts Hippo-Yap signaling and promotes proliferation of lesioned cardiac muscle cells.
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Nat Commun, 2024, 15(1):6953
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Int J Mol Sci, 2024, 25(20)11234
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bioRxiv, 2024, 2024.10.11.617852
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| E1598 |
VT103
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VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation with anti-proliferative and anti-tumor activity. It also inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation and disrupts interaction between YAP/TAZ and TEAD.
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