YAP

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).

YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor (IC50 <0.100 μΜ) for the study of abnormal immune function and cancer.

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].

YAP-TEAD-IN-1 is a competitive inhibitor of YAP–TEAD interaction (IC50: 25 nM) and exhibits higher binding affinity to TEAD1 (Kd: 15 nM) compared to YAP (50-171) (Kd: 40 nM).

YAP-TEAD-IN-1 TFA, a competitive inhibitor of the YAP–TEAD interaction (IC50: 25 nM), exhibits higher binding affinity to TEAD1 (Kd: 15 nM) compared to YAP (50-171) (Kd: 40 nM).

YAP-TEAD-IN-1 acetate is an effective and competitive inhibitor of YAP–TEAD interaction with an IC50 of 25 nM.

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.

VT104 is a potent and orally active YAP/TAZ inhibitor for cancer research. VT104 blocks palmitoylation of endogenous TEAD1 and TEAD3 proteins.

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.

VT107 is a potent pan-TEAD autopalmitoylation inhibitor. VT-107 can be used in cancer therapy research.[1]

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.

AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

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.

MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.

Super-TDU, an inhibitory peptide, targets YAP-TEADs interaction.

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.

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].

DC-TEADin02 is an inhibitor of TEAD auto palmitoylation (IC50 = 197 nM). DC-TEADin02 can be in studies about development, regeneration, and tissue homeostasis.

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.

IK-930 is an orally active TEAD inhibitor (EC50 < 0.1 µM) with potent potency.

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.

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.

K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.

YAP/TEAD-IN-1 (compound 4) is a potent inhibitor of YAP and TEAD, exhibiting antioxidant properties. It demonstrates antiproliferative effects on tumor cells while showing minimal cytotoxic activity towards normal human cells.