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-168017
    NSC682769
    		Inhibitor
    NSC682769 is a PROTAC YAP-targeting ligand (Ligands for Target Protein for PROTACs). NSC682769 can be used for synthesis PROTAC YAP degrader-1 (HY-168016).
    NSC682769
  • HY-176171
    Tubulin polymerization-IN-79
    		Inhibitor
    Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers.
    Tubulin polymerization-IN-79
  • HY-P10947
    MACTIDE-V
    		Inhibitor
    MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206+ tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.
    MACTIDE-V
  • HY-161568
    TEAD-IN-10
    		Inhibitor
    TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC50=14 nM), TEAD2 (IC50=179 nM) and TEAD3 (IC50=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research.
    TEAD-IN-10
  • HY-173076
    HDAC11-IN-1
    		Inhibitor
    HDAC11-IN-1 (Compound 14-NC6OH) is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2.
    HDAC11-IN-1
  • HY-178795
    TEAD-IN-22
    		Inhibitor
    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-183245
    51675515
    		Inhibitor
    51675515 is a YAP inhibitor that inhibits YAP-dependent transcriptional activity. 51675515 reduces YAP1-GFP intensity in cells engineered to express YAP1-GFP. 51675515 can be used for the research of YAP-dependent solid tumors (including hepatocellular carcinoma, malignant mesothelioma, colorectal cancer).
    51675515
  • HY-186021
    PROTAC TEAD degrader-2
    		Degrader
    PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma.
    PROTAC TEAD degrader-2
  • HY-161573B
    BAY-593 hydrochloride
    		Inhibitor
    BAY-593 (hydrochloride) is an orally active GGTase-I inhibitor. BAY-593 (hydrochloride) can block YAP1/TAZ signaling in animals and has antitumor activity.
    BAY-593 hydrochloride
  • HY-168085
    CV-4-26
    		Inhibitor
    CV-4-26 (Compound 22) is a covalent inhibitor of TEAD. CV-4-26 inhibits YAP/TEAD-based transcription, leading to the reduction of CTGF and CYR61 expression. CV-4-26 inhibits Huh7 and HepG2 cell colony formation, induces cell cycle arrest, and apoptosis. CV-4-26 shows antitumor activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).
    CV-4-26
  • HY-170311
    YAP/TEAD-IN-1
    		Inhibitor
    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-183753
    LC-TD-05
    		Inhibitor
    LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC50 values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC50 of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma.
    LC-TD-05
  • HY-186022
    YAP/TAZ-TEAD-IN-3
    		Inhibitor
    YAP/TAZ-TEAD-IN-3 is a YAP/TAZ-TEAD interaction inhibitor with an IC50 of 1.8 nM. YAP/TAZ-TEAD-IN-3 can be used as a TEAD1 ligand to construct PROTACs, such as PROTAC TEAD degrader-2 (HY-186021).
    YAP/TAZ-TEAD-IN-3
  • HY-159912
    pan-TEAD-IN-1
    		Inhibitor
    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-175649
    LATS1/2-IN-1
    		Inhibitor
    LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r33P functional assay. LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing.
    LATS1/2-IN-1
  • HY-182672
    VT101
    		Inhibitor
    VT101 is a TEAD inhibitor with an IC50 of 454 nM. VT101 is applicable for cancer research.
    VT101
  • HY-147209
    DC-TEAD3in03
    		Inhibitor
    DC-TEAD3in03 is a subtype-selective and covalent TEAD3 inhibitor with an IC50 of 0.16 μM. DC-TEAD3in03 exhibits the inhibitory activity on TEAD1/2/4 reduced by more than 100 times. DC-TEAD3in03 has the IC50 for TEAD3 of 1.15 μM in the GAL4-TEAD reporter gene experiment in cells, and it does not interfere with the β-catenin pathway. DC-TEAD3in03 reduces the growth rate of the zebrafish tail fin. DC-TEAD3in03 can be used to study the proportional growth of appendages in vertebrates.
    DC-TEAD3in03
  • HY-N3000A
    6-Methoxydihydrosanguinarine hydrochloride
    		Inhibitor
    6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.
    6-Methoxydihydrosanguinarine hydrochloride
  • HY-181594
    PROTAC TEAD/IAP degrader-1
    		Degrader
    PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma.
    PROTAC TEAD/IAP degrader-1
  • HY-156024
    TEAD-IN-6
    		Modulator
    TEAD-IN-6 (Example 11-1) is a TEAD modulator that blocks the interaction between YAP1/TAZ and TEAD. TEAD-IN-6 can be used in cancer research.
    TEAD-IN-6
Cat. No. Product Name / Synonyms Application Reactivity
YAP Isoform Comparison

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