TEAD activator Q2 (Quinolinol Q2) is a small molecule activator of TEAD with EC50 of 2.6 uM in TEAD dual-luciferase reporter (DLR) assays, inhibits TEAD-palmitate interaction with IC50 of 1.7 uM.

VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer.

IK930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM.

TT-10 is a novel multifaceted fluorinated compound with promising features of CM proliferative, antioxidant, and antiapoptotic activities in vitro.

TED-642 (TED642) is a potent, covalent, pan-TEAD-YAP1 antagonist, inhibits TEAD1/2/4 binding to YAP with IC50 of 0.9-1.2 uM.

TAT-PDHPS1 is an endogenous stable peptide that inhibits the proliferation of ovarian cancer cells in vitro, regulates ovarian cancer development through targeting YAP1 signaling, binds to and interacts with protein phosphatase 2 phosphatase activator (PT

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

PDHPS1 is an endogenous stable peptide which is derived from the C-terminal (2090-2110) of NUMA1, inhibits the proliferation of ovarian cancer cells in vitro, regulates ovarian cancer development through targeting YAP1 signaling, binds to and interacts wi

NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.

MYF-03-69 is a selective, covalent, irreversible TEAD inhibitor, binds with TEAD palmitate pocket, disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50=45 nM) and inhibits cell growth of defective Hippo signaling.

mCMY020 is a potent, specific and covalent inhibitor of TEAD transcriptional activity with IC50 of 91.9-468.6 nM for TEAD1-4.

LM98 (TEAD inhibitor LM98) is a flufenamic acid analogue, shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity.

AF-2112 is a small molecule inhibitor of TEAD, reduces the expression of CTGF, Cyr61, Axl and NF2, inhibits migration of human MDA-MB-231 breast cancer cells.

VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

Verteporfin(CL 318952; Visudyne), a benzoporphyrin derivative monoacid ring A, is a photosensitising drug for photodynamic therapy (PDT) activated by low-intensity, nonheat-generating light of 689nm wavelength.

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.

DC-TEADin1072 is a novel TEAD1/3 covalent inhibitor with biochemical IC50 values of 0.61 and 0.58 uM against TEAD1 and TEAD3, respectively.TEADin1072 selectively inhibited TEAD1 and TEAD3 palmitoylation while sparing TEAD2 and TEAD4.TEADin1072 demonstrated selective engagement with Cys371 of TEAD3 and Cys359 of TEAD1.

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.

Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.

Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model.