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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
T355452417718-63-7In house
VT107 is a potent pan-TEAD autopalmitoylation inhibitor. VT-107 can be used in cancer therapy research.[1]
- $147
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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.
- $116
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AICAR Cited
T14772627-69-2
AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.
- $30
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CitedMSC-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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Lats-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.
- $67
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CitedYAP-TEAD-IN-1 acetate
TP2160L1
YAP-TEAD-IN-1 acetate is an effective and competitive inhibitor of YAP–TEAD interaction with an IC50 of 25 nM.
- $147
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VT104
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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LM-41
T794272996821-30-6
LM-41, a Flufenamic acid-derived TEAD inhibitor, significantly reduces the expression of CTGF, Cyr61, Axl, and NF2, and inhibits the migration of human MDA-MB-231 breast cancer cells [1].
- $75
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IK-930
T775802563892-44-2
IK-930 is an orally active TEAD inhibitor (EC50 < 0.1 µM) with potent potency.
- $51
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VT103
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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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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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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CitedTT-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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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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AICAR 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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TED-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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YAP/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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CitedMY-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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MYF-01-37
T223722416417-65-5
MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.
- $34
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DC-TEADin02
T643422380228-45-3
DC-TEADin02 is an inhibitor of TEAD auto palmitoylation (IC50 = 197 nM). DC-TEADin02 can be in studies about development, regeneration, and tissue homeostasis.
- $31
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TEAD-IN-6
T796872821763-12-4
TEAD-IN-6 (Example 11-1) is a TEAD modulator that inhibits the YAP1 TAZ-TEAD interaction and has applications in cancer research [1].
- $1,520
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AF-2112
T79428
AF-2112, a TEAD inhibitor derived from Flufenamic acid, significantly diminishes the expression of CTGF, Cyr61, Axl, and NF2.
- $323
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YAP-TEAD-IN-2
T728882714432-83-2
YAP-TEAD-IN-2 (compound 6) is a potent inhibitor of the YAP-TEAD protein-protein interaction (PPI), with an inhibitory concentration 50 (IC50) value of 2.7 nM [1].
- $1,970
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PROTAC YAP degrader-1
T200125
PROTAC YAP degrader-1, a targeted proteolysis promoting chimeric molecule, both degrades the YAP protein and inhibits its nuclear localization. This compound is formulated with Demethyl-NSC682769 as the target protein ligand, and utilizes (R,S,R)-AHPC-PEG2-C2-boc, which is the E3 ubiquitin ligase ligand + Linker conjugate. The linker incorporated in the design is Acid-PEG2-C2-Boc.
- Inquiry Price
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CV-4-26
T200708
CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).
- Inquiry Price
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SWTX-143
T810562766575-48-6
SWTX-143, a novel covalent inhibitor, specifically and irreversibly binds to the palmitoylation pocket of all four TEAD isoforms, inhibiting the transcriptional activity of the YAP/TAZ-TEAD complex and demonstrating antitumor activity [1].
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