YAP
Yes-associated protein
YAP (Yes-associated protein) is a transcription co-activator in the Hippo tumor suppressor pathway and controls cell growth, tissue homeostasis and organ size. YAP is inhibited by the kinase Lats, which phosphorylates YAP to induce its cytoplasmic localization and proteasomal degradation. YAP induces gene expression by binding to the TEAD family transcription factors.
The function of YAP in human cancer is complex and could be cell-type-dependent. For instance, YAP could function as a tumor suppressor in some cell types, such as hematological cancers, by inducing apoptosis in response to DNA damage.
YAP Isoform Specific Products
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YAP Related Products (158)
Related Products (158)
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Antibodies (8)
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YAP Isoform Comparison
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Geranylgeranyl pyrophosphate triammonium
0 ImagesCat. No.: HY-126370ACAS No.: 313263-08-0Geranylgeranyl pyrophosphate triammonium is a type of isoprenoid metabolic intermediate, mainly synthesized through the mevalonate pathway. Geranylgeranyl pyrophosphate triammonium is a key precursor in various biological synthesis processes, especially as a necessary substrate for post-translational modification of proteins - geranylgeranyl phosphorylation. Geranylgeranyl pyrophosphate triammonium regulates various cellular processes and disease progression through protein geranylgeranyl phosphorylation, such as activating the YAP signaling pathway, promoting cell proliferation and inhibiting apoptosis; promoting IL-2 production and STAT5 phosphorylation; and influencing metabolic homeostasis and cancer, etc.
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TED-347
0 ImagesTED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
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MYF-03-69
0 ImagesSynonyms: TEAD-IN-3MYF-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).
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H122
0 ImagesCat. No.: HY-172113Purity: 98.33%H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma.
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MYF-03-176
0 ImagesMYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model.
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SWTX-143
0 ImagesSWTX-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.
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IBS008738
0 ImagesIBS008738 is a potent TAZ activator. IBS008738 stabilizes TAZ, increases the unphosphorylated TAZ level, enhances the association of MyoD with the myogenin promoter, upregulates MyoD-dependent gene transcription, and competes with myostatin in C2C12 cells. IBS008738 enhances myogenesis in C2C12 cells and facilitates muscle repair in a muscle injury model.
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PROTAC YAP degrader-1
0 ImagesPROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma.
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α-Ionone
0 Imagesα-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro.
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TEAD1/3/4-IN-1
0 ImagesTEAD1/3/4-IN-1 is an orally active inhibitor of TEAD1/3/4. TEAD1/3/4-IN-1 inhibits the YAP/TAZ-TEAD interaction, with its EC50 being 2 nM. TEAD1/3/4-IN-1 has anti-proliferative activity against NCI-H226 cells. TEAD1/3/4-IN-1 can be used in the research of lung squamous cell carcinoma.
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HTH-02-006
0 ImagesCat. No.: HY-156397Purity: 99.42%HTH-02-006 is a NUAK2 inhibitor, with an IC50 value of 126 nM. HTH-02-006 inhibits NUAK2-mediated signaling by reducing phosphorylation of its substrate MYPT1 at S445 and downstream MLC. HTH-02-006 shows growth inhibitory efficacy in YAP-high cancer cells (HuCCT-1, SNU475). HTH-02-006 significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice and demonstrates significant anti-tumor efficacy in mice bearing HMVP2 prostate cancer allografts. HTH-02-006 can be used for the study of liver cancer and prostate cancer.
