1. Signaling Pathways
  2. Stem Cell/Wnt
  3. YAP

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161443
    TEAD-IN-9
    Inhibitor
    TEAD-IN-9 (compound 17) is a TEAD1 inhibitor with an IC50 of 0.29 μM. TEAD-IN-9 targets the palmitoyl pocket of TEAD, thereby effectively inhibiting the binding of YAP-TEAD and blocking the transcriptional function of YAP-TEAD.
    TEAD-IN-9
  • HY-181537
    PROTAC TEAD1/IAP degrader-2
    Degrader
    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
  • HY-126370
    Geranylgeranyl pyrophosphate
    Activator
    Geranylgeranyl pyrophosphate is a type of isoprenoid metabolic intermediate, mainly synthesized through the mevalonate pathway. Geranylgeranyl pyrophosphate is a key precursor in various biological synthesis processes, especially as a necessary substrate for post-translational modification of proteins - geranylgeranyl phosphorylation. Geranylgeranyl pyrophosphate 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.
    Geranylgeranyl pyrophosphate
  • HY-182743
    OICR19451
    Activator
    OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer.
    OICR19451
  • HY-147165A
    VT02956 hydrochloride
    Inhibitor
    VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VT02956 hydrochloride
  • HY-181539
    TEAD ligand-Linker Conjugate 2
    TEAD ligand-Linker Conjugate 2 (compound S24) is a conjugate of TEAD‑targeted ligand and linker, which can be used for the synthesis of PROTAC TEAD1/IAP degrader-2 (HY-181537).
    TEAD ligand-Linker Conjugate 2
  • HY-13285R
    Ki16425 (Standard)
    Inhibitor
    Ki16425 (Standard) is the analytical standard of Ki16425. This product is intended for research and analytical applications. Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
    Ki16425 (Standard)
  • HY-180514
    TEAD-IN-24
    Inhibitor
    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-160657
    DC-TEADin04
    DC-TEADin04 has weak inhibitory activity against TEAD4 palmitoylation.
    DC-TEADin04
  • HY-157083
    mCMY020
    Inhibitor
    mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research.
    mCMY020
  • HY-169316
    YAP/TAZ inhibitor-4
    Inhibitor
    YAP/TAZ inhibitor-4 (Compound 45) is an inhibitor of YAP/TAZ, exhibiting TEAD transcriptional activation inhibitory activity by suppressing the binding of YAP or TAZ to TEAD.
    YAP/TAZ inhibitor-4
  • HY-168505
    MSC-5046
    Inhibitor
    MSC-5046 is a selective TEAD1 inhibitor.
    MSC-5046
  • HY-181607
    TEAD ligand-Linker Conjugate 3
    Degrader
    TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors.
    TEAD ligand-Linker Conjugate 3
  • HY-181538
    TEAD ligand 3
    Ligand
    TEAD ligand 3 (compound S20) is a TEAD ligand. As a target protein ligand, TEAD ligand 3 can be used in the synthesis of PROTAC TEAD1/IAP degrader-2 (HY-181537).
    TEAD ligand 3
  • HY-163732
    TEAD-IN-16
    Inhibitor
    TEAD-IN-16 (compound BC-011) is a potent inhibitor of TEAD, with the IC50 of 72.43 μM. TEAD-IN-16 plays an important role in cancer research.
    TEAD-IN-16
Cat. No. Product Name / Synonyms Application Reactivity

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