YAP Inhibitor

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma.

Liposomal verteporfin is a liposome-encapsulated form of Verteporfin (HY-B0146). Verteporfin is a photosensitizer used in photodynamic therapy, which generates reactive oxygen species (ROS) upon irradiation at 690 nm to mediate photodynamic effects. Liposomal verteporfin can promote the release of Oxaliplatin (HY-17371) from endolysosomes via photochemical internalization (PCI), prolong the drug circulation time and enable sustained release, accumulate the drug in neovascular vessels, and enhance its cytotoxicity in tumor models. Liposomal verteporfin can be used in studies related to neovascular eye diseases and pancreatic cancer^[1][2][3].

VT104 is a potent and orally active YAP/TAZ inhibitor. VT104 prevents palmitoylation of endogenous TEAD1 and TEAD3 proteins. VT104 can be used in research of cancer.

IK-930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC₅₀ value of <0.1 µM.

VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer.

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.

MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC₅₀ of 11 nM. The IC₅₀ values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model.

VT-105 is a TEAD inhibitor and VT104 (HY-134956) analog. VT-105 binds to the central hydrophobic pocket of the TEAD3 protein. VT-105 can be used in the research of NF2-deficient malignant mesothelioma.

Pipecolic acid (Standard) is the analytical standard of Pipecolic acid. This product is intended for research and analytical applications. Pipecolic acid is a metabolite of lysine and an important precursor for many useful microbial secondary metabolites. Pipecolic acid slows ferroptosis in diabetic retinopathy by inhibiting the YAP-GPX4 signaling pathway. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxine-dependent epilepsy.

AICAR (Standard) is the analytical standard of AICAR. This product is intended for research and analytical applications. AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.

TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD.

MY-1076 is an inhibitor of YAP. MY-1076 induces YAP degradation and cell apoptosis. MY-1076 inhibits MGC-803, SGC-7901, HCT-116 and KYSE450 cells proliferation with IC₅₀ s of 0.019, 0.017, 0.020 and 0.044 μM, respectively.

6-Methoxydihydrosanguinarine is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine 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 induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.

YAP-TEAD-IN-2 (compound 6) is a potent YAP-TEAD PPI (protein-protein interaction) inhibitor with IC₅₀ is 2.7 nM.

LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells.

DC-TEADin02 is a potent TEAD autopalmitoylation inhibitor. DC-TEADin02 has TEAD autopalmitoylation inhibitory with the IC₅₀ value of 197 nM. DC-TEADin02 can be used for the research of development, regeneration and tissue homeostasis.

KHKI-01215 is an inhibitor for NUAK2 with an IC₅₀ of 0.052 μM. KHKI-01215 inhibits the proliferation of cancer cell SW480 with an IC₅₀ of 3.16 μM, induces apoptosis in SW480. KHKI-01215 inhibits the YAP signaling pathway.

TEAD-IN-11 (compound 38) has a good inhibitory effect on TEAD1 (IC₅₀=8.7 nM), TEAD2 (IC₅₀=3.4 nM), TEAD3 (IC₅₀=5.6 nnM). TEAD-IN-11 has good selective activity against TEAD1-3 as a covalent inhibitor. TEAD-IN-11 can be used for cancer research.

YAP/TEAD-IN-2 (Compound T-1) is a YAP/TEAD inhibitor. YAP/TEAD-IN-2 inhibits the luciferase activity driven by YAP/TEAD in 293T cells. YAP/TEAD-IN-2 exhibits strong anti-proliferative activity against human pleural mesothelioma NCI-H226 cells. YAP/TEAD-IN-2 can be used for the study of diseases associated with Hippo pathway dysregulation, particularly cancers.