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Stem CellsYAP
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.
Verteporfin
Cited
T3112129497-78-5
Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.
- $34
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CitedYAP-TEAD-IN-3
T777252714434-21-4
YAP-TEAD-IN-3 is an inhibitor of YAP/TAZ-TEAD interactions with an IC50 of 9 nM for Avi-human TEAD (4217-434). YAP-TEAD-IN-3 inhibits YAP reporter gene expression (IC50 = 0.048 μM) and NCI-H2052 cell proliferation (IC50 = 0.048 μM).
- $328
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vt107 Cited
T355452417718-63-7In house
VT107 is a potent pan-TEAD autopalmitoylation inhibitor. VT-107 can be used in cancer therapy research.[1]
- $132
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CitedCytochalasin D
T322922144-77-0
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
- $239
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PY-60
T95662765218-56-0
PY-60 can effectively activate YAP transcriptional activity against annexin A2 (ANXA2) (Kd value of 1.4 µM). PY-60 activates a pro-proliferative, YAP-dependent transcriptional program in adult animals that are able to remodel the epidermis through proliferation.
- $52
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AICAR Cited
T14772627-69-2
AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.
- $30
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CitedLats-IN-1 Cited
T90531424635-83-5
Lats-IN-1 is a potent and ATP-competitive Lats1 and Lats2 kinases inhibitor. It promotes Yap-dependent proliferation in postmitotic mammalian tissues.
- $58
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CitedTDI-011536
T601442687970-96-1
TDI-011536, a potent Lats kinase inhibitor, disrupts Hippo-Yap signaling and promotes the proliferation of lesioned heart muscle cells. This compound is valuable for research in organ conservation and regeneration.
- $51
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LM-41
T794272996821-30-6
LM-41 is a TEAD-binding agent with potential anticancer activity that strongly reduces the expression of CTGF, Cyr61, Axl and NF2, and can be used in the study of breast cancer.
- $75
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MSC-4106
T601482738542-58-8
MSC-4106, an orally active and potent YAP TAZ-TEAD inhibitor, disrupts TEAD1 and TEAD3 auto-palmitoylation and demonstrates significant efficacy in the NCI-H226 tumor xenograft model [1].
- $97
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GNE-7883
T785582648450-42-2
GNE-7883 is an inhibitor targeting TEAD transcription factor, inhibits cell proliferation and suppresses YAP/TAZ activation, and can be used to study YAP/TAZ-dependent tumors.
- $118
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GA-017
T600132351906-74-4
GA-017 is a potent, selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1/2), exhibiting IC50 values of 4.10 and 3.92 nM, respectively. This compound simultaneously acts as an activator of cell proliferation by promoting YAP/TAZ activation and their nuclear translocation. Additionally, GA-017 enhances cell growth in 3D culture conditions and augments the ex vivo formation of mouse intestinal organoids [1].
- $98
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ML-7 hydrochloride Cited
T3050110448-33-4
ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.
- $30
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CitedTED-347
T84212378626-29-8
TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.
- $78
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K-975
T99542563855-03-6
K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1 TAZ.
- $67
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TT-10
T697602230640-94-3
TT-10 (TAZ-K), an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity, has potential application in heart disease research, specifically for conditions characterized by loss of cardiomyocytes.
- $34
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NIBR-LTSi
T201369
NIBR-LTSi is a selective LATS kinase inhibitor that also activates YAP signaling, promotes tissue stem cell expansion and tissue regeneration both in vitro and in vivo, accelerates liver regeneration in a mouse partial hepatectomy model, and is capable of expanding organoids derived from several mouse and human tissues.
- $79
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YAP/TAZ inhibitor-2
T602182762617-31-0
YAP/TAZ inhibitor-2 is a potent, orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM, demonstrating anti-proliferative and antitumor activity [1].
- $84
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VT103 Cited
T620772290608-13-6In house
VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer.
- $126
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CitedVT104
T678722417718-25-1
VT104 is a potent and orally active YAP/TAZ inhibitor for cancer research. VT104 blocks palmitoylation of endogenous TEAD1 and TEAD3 proteins.
- $72
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IK-930 Cited
T775802563892-44-2
IK-930 is an orally active TEAD inhibitor (EC50 < 0.1 µM) with potent potency.
- $51
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CitedYAP/TAZ inhibitor-1 Cited
T133642093565-23-0
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor (IC50 <0.100 μΜ) for the study of abnormal immune function and cancer.
- $487
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CitedAICAR phosphate
T14149681006-28-0
AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.
- $49
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MY-1076
T777293008262-76-5
MY-1076 is a potent YAP inhibitor with antigastric cancer activity.MY-1076 dose-dependently induced G2 M phase block, induced YAP degradation and apoptosis, and inhibited microtubule protein polymerization.MY-1076 inhibited the proliferation of MGC-803, SGC-7901, HCT-116, and KYSE450 cells.
- $30
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