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-158395
    TEAD-IN-13
    Inhibitor
    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-158394
    TEAD-IN-12
    Inhibitor
    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-B0146R
    Verteporfin (Standard)
    Inhibitor
    Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
    Verteporfin (Standard)
  • HY-161611
    14-3-3-IN-1
    14-3-3-IN-1 (Compound 2) is an inhibitor for 14-3-3 proteins in Arabidopsis thaliana, with an IC50 of 1.21 μM. 14-3-3-IN-1 exhibits different inhibitory activities against different 14-3-3 isomers. 14-3-3-IN-1 promotes the closure of stomata on leaves.
    14-3-3-IN-1
  • HY-E70293
    N-Acetylgalactosaminyltransferase 12
    N-Acetylgalactosaminyltransferase 12 (GALNT12) belongs to the uridine diphosphate N-acetylgalactosamine gene family and is involved in the biological processes of many diseases, such as tumor progression. N-Acetylgalactosaminyltransferase 12 is a potential biomarker for fibrosarcoma, and its high expression level is closely related to the yes1-associated transcriptional regulator (YAP1) signaling pathway.
    N-Acetylgalactosaminyltransferase 12
  • HY-170936
    MY-1576
    Inhibitor
    MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo.
    MY-1576
  • HY-P1727A
    Super-TDU TFA
    Antagonist
    Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model.
    Super-TDU TFA
  • HY-158396
    TEAD-IN-14
    Inhibitor
    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-173139
    TEAD-IN-19
    Inhibitor
    TEAD-IN-19 (Compound 1l) is a transcriptional inhibitor of TEAD, exhibiting inhibition rates of 38.5%, 36.2%, 57.8%, and 71.3% against TEAD1, TEAD2, TEAD3, and TEAD4, respectively, at a concentration of 10 μM. TEAD-IN-19 shows potent anti-proliferative and anti-migratory activities in prostate cancer cell lines and significantly reduces the expression of TEAD-regulated downstream genes. TEAD-IN-19 holds promise for research in the field of cancer therapy.
    TEAD-IN-19
  • HY-162126
    Tubulin polymerization-IN-58
    Degrader
    Tubulin polymerization-IN-58 (Compound K18) is a tubulin polymerization inhibitor with an IC50 of 0.446 μM. Tubulin polymerization-IN-58 also induces the degradation of oncogenic protein YAP via the UPS pathway, thus can be used for cancer research.
    Tubulin polymerization-IN-58
  • 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-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-P11219
    TAT-PDHPS1
    Inhibitor
    TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research.
    TAT-PDHPS1
  • 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
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