YAP Inhibitor

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.

SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity.

BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.

YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC₅₀=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (K_d=15 nM) than YAP (50-171) (K_d=40 nM).

TEAD1/3/4-IN-1 is an orally active inhibitor of TEAD1/3/4. TEAD1/3/4-IN-1 inhibits the YAP/TAZ-TEAD interaction, with its EC₅₀ being 2 nM. TEAD1/3/4-IN-1 has anti-proliferative activity against NCI-H226 cells. TEAD1/3/4-IN-1 can be used in the research of lung squamous cell carcinoma.

HTH-02-006 is a NUAK2 inhibitor, with an IC₅₀ value of 126 nM. HTH-02-006 inhibits NUAK2-mediated signaling by reducing phosphorylation of its substrate MYPT1 at S445 and downstream MLC. HTH-02-006 shows growth inhibitory efficacy in YAP-high cancer cells (HuCCT-1, SNU475). HTH-02-006 significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice and demonstrates significant anti-tumor efficacy in mice bearing HMVP2 prostate cancer allografts. HTH-02-006 can be used for the study of liver cancer and prostate cancer.

YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC₅₀ value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity.

YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC₅₀=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (K_d=15 nM) than YAP (50-171) (K_d= 40 nM).

MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction.

Pipecolic acid-d₉ is the deuterium labeled Pipecolic acid. 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.

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor 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.

TEAD-IN-1 (Compound 2) is potent TEAD autopalmitoylation inhibitor, with an IC₅₀ of 603 nM. TEAD-IN-1 increases the interaction of TEAD and VGLL4. TEAD-IN-1 decreases the interaction of YAP and TEAD. TEAD-IN-1 can be used for the research of cancer.

LATS-IN-2 is an efficiently acting LATS (large tumor suppressor kinase) inhibitor. LATS-IN-2 shows potent inhibitory activity against LATS1 with an IC₅₀ value of 1.3 nM. LATS-IN-2 suppresses the phosphorylation of YAP by inhibiting LATS kinase activity. LATS-IN-2 increases the thickness of the epidermis in mice. LATS-IN-2 can be used for the study of ocular diseases such as limbal stem cell deficiency and corneal endothelial dysfunction.

TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC₅₀ of 5.1 nM and a K_i of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer.