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Results for "

tead+inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-153811
    IAG933
    3 Publications Verification

    YAP-TEAD-IN-3

    		 YAP Apoptosis Cancer
    IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD 4217-434, with an IC50 value of 9 nM .
    IAG933
  • HY-138565
    K-975
    Maximum Cited Publications
    31 Publications Verification

    		 YAP Cancer
    K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
    K-975
  • HY-147214
    GNE-7883
    5 Publications Verification

    		 YAP Cancer
    GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
    GNE-7883
  • HY-153585
    IK-930
    4 Publications Verification

    		 YAP Cancer
    IK-930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM .
    IK-930
  • HY-155338
    SWTX-143

    		YAP Cancer
    SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
    SWTX-143
  • HY-175357
    YAP/TEAD-IN-2

    		YAP Cancer
    YAP/TEAD-IN-2 (Compound T-1) is a YAP/TEAD inhibitor. YAP/TEAD-IN-2 inhibits the luciferase activity driven by YAP/TEAD in 293T cells. YAP/TEAD-IN-2 exhibits strong anti-proliferative activity against human pleural mesothelioma NCI-H226 cells. YAP/TEAD-IN-2 can be used for the study of diseases associated with Hippo pathway dysregulation, particularly cancers .
    YAP/TEAD-IN-2
  • HY-147135
    MYF-03-69
    1 Publications Verification

    TEAD-IN-3

    		 YAP Apoptosis Cancer
    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) .
    MYF-03-69
  • HY-139603
    MYF-01-37
    1 Publications Verification

    		 YAP Cancer
    MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction .
    MYF-01-37
  • HY-163644
    VT-105

    		YAP Cancer
    VT-105 is a TEAD inhibitor and VT104 (HY-134956) analog. VT-105 binds to the central hydrophobic pocket of the TEAD3 protein. VT-105 can be used in the research of NF2-deficient malignant mesothelioma .
    VT-105
  • HY-155310
    AF-2112

    		YAP Cancer
    AF-2112 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2.
    AF-2112
  • HY-163173
    TEAD-IN-8

    		YAP Cancer
    TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
    TEAD-IN-8
  • HY-155309
    LM-41

    		YAP Cancer
    LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
    LM-41
  • HY-178795
    TEAD-IN-22

    		YAP Inflammation/Immunology Cancer
    TEAD-IN-22 (compound I) is a TEAD inhibitor. TEAD-IN-22 has the potential for the research of cancer and fibrosis .
    TEAD-IN-22
  • HY-158395
    TEAD-IN-13

    		YAP Cancer
    TEAD-IN-13 (64) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.2 h in mouse .
    TEAD-IN-13
  • HY-179505
    OPN-9652

    		YAP Cancer
    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 .
    OPN-9652
  • HY-179395
    TEAD-IN-23

    		YAP Cancer
    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 .
    TEAD-IN-23
  • HY-179440
    EA-C15

    		YAP Cancer
    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 .
    EA-C15
  • HY-168704
    YAP/TAZ-TEAD-IN-2

    		YAP TAM Receptor Survivin Cancer
    YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
    YAP/TAZ-TEAD-IN-2
  • HY-178098
    TEAD-IN-21

    		YAP Cancer
    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) .
    TEAD-IN-21
  • HY-159912
    pan-TEAD-IN-1

    		YAP Cancer
    pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
    pan-TEAD-IN-1
  • HY-158396
    TEAD-IN-14

    		YAP Cancer
    TEAD-IN-14 (75a) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 2.3 h in mouse .
    TEAD-IN-14
  • HY-158394
    TEAD-IN-12

    		YAP Cancer
    TEAD-IN-12 (58B) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.6 h in mouse .
    TEAD-IN-12
  • HY-172932
    TEAD-IN-20

    		YAP Cancer
    TEAD-IN-20 is a TEAD inhibitor. The IC50 values of TEAD-IN-20 in TEAD4 FRET and TEAD4 MCF7-Tead cell lines are 0.021 and 0.044 μM, respectively. TEAD-IN-20 can be used in cancer research .
    TEAD-IN-20
  • HY-170311
    YAP/TEAD-IN-1

    		YAP Cancer
    YAP/TEAD-IN-1 (compound 4) is a potent YAP and TEAD inhibitor. YAP/TEAD-IN-1 shows antioxidant activity. YAP/TEAD-IN-1 shows antiproliferation activity for tumor cells. YAP/TEAD-IN-1 shows little cytotoxic activity for human normal cells .
    YAP/TEAD-IN-1
  • HY-182672
    VT101

    		YAP Cancer
    VT101 is a TEAD inhibitor with an IC50 of 454 nM. VT101 is applicable for cancer research .
    VT101
  • HY-180514
    TEAD-IN-24

    		YAP Cancer
    TEAD-IN-24 (Example 65) is a TEAD inhibitor. TEAD-IN-24 exhibits anti-cancer activity against non-small cell lung cancer .
    TEAD-IN-24
  • HY-183728
    LC-TEAD01

    		YAP Cancer
    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 .
    LC-TEAD01
  • HY-181537
    PROTAC TEAD1/IAP degrader-2

    		PROTACs SNIPERs YAP IAP Cancer
    PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .
    PROTAC TEAD1/IAP degrader-2

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