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.

Verteporfin liposome is a liposome-encapsulated form of Verteporfin (HY-B0146). Verteporfin is a photosensitizer used in photodynamic therapy to eliminate abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin liposome prolongs drug circulation time and provides slow release, allowing the drug to accumulate in newly formed blood vessels.

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.