| E6486New |
VT3989
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VT3989 (YAP/TAZ inhibitor-3) is a potent and selective oral inhibitor of TEAD auto-palmitoylation, blocking its interaction with yes-associated protein (YAP). It exhibits antitumor activity and shows potential for treating mesothelioma and solid tumors with NF2 mutations.
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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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| S9735 |
MGH-CP1
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MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation. This compound exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.
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EMBO Rep, 2024, 25(9):4033-4061
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Sci Adv, 2023, 9(1):eadd0960
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Sci Adv, 2023, 9(28):eadf9460
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| E1329 |
K-975
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K-975 is a potent, selective and orally active TEAD inhibitor that directly inhibits YAP/TAZ-TEAD protein-protein interaction and shows a potent anti-tumor effect in malignant pleural mesothelioma.
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Nat Commun, 2024, 15(1):8159
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iScience, 2024, 27(3):109247
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| S8950 |
MYF-01-37
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MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein.
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Exp Dermatol, 2022, 31(10):1477-1499
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| E1599 |
VT107
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VT107 is an enantiomer analogous to VT10 and is a potent inhibitor of pan-TEAD auto-palmitoylation with IC50 of 4.93 nM that blocks TEAD-mediated gene transcription by preventing its association with YAP/TAZ.
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Mol Oncol, 2024, 10.1002/1878-0261.13749
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| E1483 |
IK-930
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IK-930 is a selective, small-molecule inhibitor of TEAD that prevents palmitate binding and thereby disrupts aberrant TEAD-dependent transcription. This compound demonstrates antitumor activity in mouse xenograft models with Hippo pathway genetic alterations.
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| E6434New |
BPI-460372
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BPI‑460372 is an orally available, covalent, irreversible inhibitor of TEAD 1/3/4 that binds to the cysteine residue in the TEAD palmitoylation pocket, preventing palmitoylation and inhibiting TEAD’s transcriptional activity.
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| E4655 |
VT104
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VT104 is an inhibitor of TEAD auto-palmitoylation that effectively blocks the palmitoylation of TEAD1 and TEAD3 proteins. It selectively inhibits YAP/TAZ-TEAD-promoted gene transcription and exhibits strong antitumor and anti-proliferative effects.
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