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

YAP

Yes-associated protein

YAP

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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:

YAP Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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).
    TEAD ligand 1
  • HY-181530
    IAP ligand 6
    		Ligand
    IAP ligand 6 (A250) is an IAP ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534).
    IAP ligand 6
  • 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) .
    TEAD ligand 4
  • 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.
    M3686
  • HY-13417S
    AICAR-13C2,15N
    		Inhibitor
    AICAR-13C2,15N (Acadesine-13C2,15N; AICA Riboside-13C2,15N) is the 13C and 15N labeled AICAR (HY-13417). AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
    AICAR-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-172932
    TEAD-IN-20
    		Inhibitor
    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-162012
    HC-258
    HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells.
    HC-258
  • HY-185230
    HC278
    		Degrader
    HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma.
    HC278
  • 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.
    PROTAC TEAD1/IAP degrader-1
  • 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).
    TEAD-IN-21
  • 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) .
    TEAD ligand 5
  • HY-179165
    Gαq/11 protein-IN-2
    		Activator
    Gαq/11 protein-IN-2 (Compound 9g) is a Gαq/11 protein inhibitor, with an IC50 of 11.3 μM. Gαq/11 protein-IN-2 induces Apoptosis, increases p-YAP. Gαq/11 protein-IN-2 has anticancer activity against uveal melanoma.
    Gαq/11 protein-IN-2
  • 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.
    LC-TEAD01
  • 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.
    OPN-9643
  • HY-179706
    VS3
    		Inhibitor
    VS3 is a YAP-TEAD interaction inhibitor. VS3 directly disrupts the interaction between YAP-TEAD by binding to TEAD4 Interface 3 (Kd = 6 μM) on the surface. VS3 exhibits anti-proliferative activity against HT29, HCT116, and A2780. VS3 can be used for research on colorectal adenocarcinoma and ovarian cancer.
    VS3
  • 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.
    EA-C15
  • HY-168506
    MSC-1254
    		Inhibitor
    MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer.
    MSC-1254
  • HY-168704
    YAP/TAZ-TEAD-IN-2
    		Inhibitor
    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-176548
    PY-PAP
    		Activator
    PY-PAP is a photoactivatable affinity probe and a derivative of PY-60 (HY-141644). PY-PAP retains the cellular function of activating YAP transcriptional activity. In 293A cells, PY-PAP can label cathepsin D (CTSD) and annexin A2 (ANXA2) through ultraviolet crosslinking and click reactions. PY-PAP plays a key role in identifying ANXA2 as the specific target of PY-60.
    PY-PAP
  • HY-175538
    USP10-IN-4
    		Inhibitor
    USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC50 of 10.87 μM and a Kd of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC).
    USP10-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
YAP Isoform Comparison

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