2. Signaling Pathways
  3. Stem Cell/Wnt
  4. YAP
  5. TEAD Isoform

TEAD

TEAD (TEA domain) transcription factors comprise a highly conserved family of DNA-binding proteins that function as the major transcriptional effectors of the Hippo signaling pathway and regulate cell growth, proliferation, tissue homeostasis, regeneration, and embryonic development[1][2]. Mechanistically, TEAD proteins bind genomic target sequences and cooperate with the transcriptional coactivators YAP and TAZ to control transcriptional programs that govern cellular proliferation, differentiation, and survival[1][3]. Through this YAP/TAZ-TEAD transcriptional module, Hippo pathway activity is translated into gene-expression outputs that influence developmental processes and organ homeostasis[1][4]. In disease contexts, increased TEAD transcriptional activity has been associated with tumorigenesis and therapeutic resistance, and dysregulated Hippo signaling can promote TEAD-dependent oncogenic transcription in multiple cancer types[3][5][6]. Experimental studies further demonstrate that disruption of YAP-TEAD interactions suppresses YAP-dependent gene expression and oncogenic transformation, supporting TEAD as a critical functional node in cancer biology[3]. Compared with related family members, TEAD1, TEAD3, and TEAD4 are broadly expressed in multiple adult tissues, whereas TEAD2 displays a more restricted embryonic expression pattern and is largely absent from adult tissues, indicating distinct biological roles despite strong structural conservation[7]. Research on TEAD-targeted therapeutics has therefore focused on inhibitors that disrupt TEAD-mediated transcriptional complexes or directly antagonize TEAD activity, providing valuable experimental tools for investigating Hippo pathway function and evaluating anticancer strategies[5][8][9].

TEAD Related Products (35):

Cat. No. Product Name Effect Purity
  • HY-147135
    MYF-03-69
    		Inhibitor 98.11%
    MYF-03-69 (TEAD-IN-3) is a covalent and irreversible TEAD inhibitor with IC50s of 385, 143, 558 and 173 nM for TEAD1, TEAD2, TEAD3 and TEAD4. MYF-03-69 disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50 = 56 nM) and up-regulates apoptosis gene BMF. MYF-03-69 selectively inhibits mesothelioma cancer cells with defective Hippo signaling. MYF-03-69 can be used for the study of malignant pleural mesothelioma (MPM).
  • HY-158342
    PROTAC TEAD degrader-1
    		Degrader 99.82%
    PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer.
  • HY-137479
    TEAD-IN-1
    		Inhibitor 99.43%
    TEAD-IN-1 (Compound 2) is potent TEAD autopalmitoylation inhibitor, with an IC50 of 603 nM. TEAD-IN-1 increases the interaction of TEAD and VGLL4. TEAD-IN-1 decreases the interaction of YAP and TEAD. TEAD-IN-1 can be used for the research of cancer.
  • HY-186117
    KG-FP-003
    		Degrader
    KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer.
  • HY-181536
    TEAD ligand 2
    		Ligand
    TEAD ligand 2 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534). PROTAC TEAD1/IAP degrader-1 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity.
  • HY-181592
    TEAD ligand 4
    		Degrader
    TEAD ligand 4 is a TEAD PROTAC ligand. TEAD ligand 4 can be conjugated with E3 ligase Ligand (HY-181591) and linker to synthesize PROTAC TEAD1/IAP degrader (HY-181590) .
  • HY-158400
    TEAD ligand 1
    TEAD ligand 1 is the ligand for target protein TEAD. TEAD ligand 1 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342).
  • HY-170764
    M3686
    		Inhibitor
    M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model.
  • HY-179505
    OPN-9652
    		Inhibitor 98.84%
    OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research.
  • HY-181534
    PROTAC TEAD1/IAP degrader-1
    		Degrader
    PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.
  • HY-178098
    TEAD-IN-21
    		Inhibitor
    TEAD-IN-21 is a potent and orally active pan-TEAD inhibitor with an IC50 of 3 nM. TEAD-IN-21 effectively inhibited the proliferation of Huh-7 cells. TEAD-IN-21 selectively downregulates TEAD-dependent downstream genes. TEAD-IN-21 achieves tumor regression in a liver cancer-derived tumor xenograft mice model. TEAD-IN-21 can be used in the research of hepatocellular carcinoma (HCC).
  • HY-181595
    TEAD ligand 5
    		Ligand
    TEAD ligand 5 (Compound S19) is a TEAD PROTAC ligand. TEAD ligand 5 can be conjugated with E3 ligase Ligand (HY-181531) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
  • HY-183728
    LC-TEAD01
    		Inhibitor
    LC-TEAD01 is a potent covalent transcription enhancer-associated domain (TEAD) inhibitor with an IC50 of 116 nM and a Ki of 0.132 μM. LC-TEAD01 disrupts the TEAD-YAP interaction and inhibits TEAD-dependent transcriptional activity. LC-TEAD01 suppresses the proliferation of NF2-deficient cancer cells. LC-TEAD01 inhibits tumor growth in NF2-deficient xenograft models. LC-TEAD01 can be used in studies related to NF2-deficient malignant pleural mesothelioma.
  • HY-179559
    OPN-9643
    		Inhibitor
    OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma.
  • HY-179440
    EA-C15
    		Inhibitor
    EA-C15 is a potent and selective TEAD inhibitor with an IC50 of 0.34 μM. EA-C15 covalently binds to the TEAD palmitoylation site, blocks palmitoylation and transcriptional activity, and inhibits YAP-dependent cancer cell proliferation and YAP-TEAD target gene (CTGF and CYR61) transcription. EA-C15 can be used for cancer research.
  • HY-182673
    VT102
    		Inhibitor
    VT102 is a TEAD1 inhibitor with a human IC50 of 391 nM. VT102 inhibits auto-palmitoylation, attenuates YAP/TEAD1 interaction, reduces expression of TEAD target genes, and inhibits YAP-mediated luciferase reporter activity. VT102 exerts weak cell growth inhibitory activity in cancer cells. VT102 can be used for the research of cancer.
  • HY-179395
    TEAD-IN-23
    		Inhibitor
    TEAD-IN-23 (Compound 22) is an efficient pan-TEAD inhibitor with an IC50 of 10 nM. TEAD-IN-23 exhibits potent anti-proliferative activity in both NCI-H226 and MSTO-211H. TEAD-IN-23 causes complete tumor regression in the MSTO-211H xenograft tumor model. TEAD-IN-23 can be used for the study of mesothelioma and hepatocellular carcinoma.
  • HY-181590
    PROTAC TEAD1/IAP degrader-3
    		Degrader
    PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma.
  • HY-184179
    TEAD degrader-1
    		Degrader
    TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC50 of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer.
  • HY-186023
    TEAD ligand-Linker Conjugate 1
    TEAD ligand-Linker Conjugate 1 is a synthetic target protein ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC TEAD degrader-2 (HY-186021). PROTAC TEAD degrader-2 is a potent TEAD1 PROTAC degrader with anti-cancer activity.