YAP Inhibitor

AF-2112 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2.

HDAC11-IN-1 (Compound 14-N^C6OH) TFA is a selective macrocyclic inhibitor of HDAC11 with a K_i of 40 nM. HDAC11-IN-1 TFA exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2.

(R)-VT104 is the R-enantiomer of VT104. (R)-VT104 shows an IC₅₀ value of 0.1-1 μΜ for firefly luciferase. VT104 is an orally active and pan-TEAD auto-palmitoylation inhibitor.

(R,S)-YAP-TEAD-IN-2 is the racemic mixture of YAP-TEAD-IN-2 (HY-151525). YAP-TEAD-IN-2 (Compound 6) is a potent inhibitor of YAP-TEAD PPIs (protein-protein interaction) with an IC₅₀ of 2.7 nM.

TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research.

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

AICAR-¹³C₂,¹⁵N (Acadesine-¹³C₂,¹⁵N; AICA Riboside-¹³C₂,¹⁵N) is the ¹³C and ¹⁵N labeled AICAR (HY-13417). 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-20 is a TEAD inhibitor. The IC₅₀ values of TEAD-IN-20 in TEAD4 FRET and TEAD4 MCF7-Tead cell lines are 0.021 and 0.044 μM, respectively. TEAD-IN-20 can be used in cancer research.

VS3 is a YAP-TEAD interaction inhibitor. VS3 directly disrupts the interaction between YAP-TEAD by binding to TEAD4 Interface 3 (K_d = 6 μM) on the surface. VS3 exhibits anti-proliferative activity against HT29, HCT116, and A2780. VS3 can be used for research on colorectal adenocarcinoma and ovarian cancer.

MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer.

TEAD-IN-13 (64) is an orally active TEAD inhibitor, with an IC₅₀ of <100 nM and a half-life of 3.2 h in mouse.

TEAD-IN-12 (58B) is an orally active TEAD inhibitor, with an IC₅₀ of <100 nM and a half-life of 3.6 h in mouse.

TEAD-IN-14 (75a) is an orally active TEAD inhibitor, with an IC₅₀ of <100 nM and a half-life of 2.3 h in mouse.

TEAD-IN-19 (Compound 1l) is a transcriptional inhibitor of TEAD, exhibiting inhibition rates of 38.5%, 36.2%, 57.8%, and 71.3% against TEAD1, TEAD2, TEAD3, and TEAD4, respectively, at a concentration of 10 μM. TEAD-IN-19 shows potent anti-proliferative and anti-migratory activities in prostate cancer cell lines and significantly reduces the expression of TEAD-regulated downstream genes. TEAD-IN-19 holds promise for research in the field of cancer therapy.

NSC682769 is a PROTAC YAP-targeting ligand (Ligands for Target Protein for PROTACs). NSC682769 can be used for synthesis PROTAC YAP degrader-1 (HY-168016).

Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC₅₀=0.36 μM; EC-109, IC₅₀=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers.

MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206⁺ tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.

TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC₅₀=14 nM), TEAD2 (IC₅₀=179 nM) and TEAD3 (IC₅₀=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research.

TEAD-IN-22 (compound I) is a TEAD inhibitor. TEAD-IN-22 has the potential for the research of cancer and fibrosis.

51675515 is a YAP inhibitor that inhibits YAP-dependent transcriptional activity. 51675515 reduces YAP1-GFP intensity in cells engineered to express YAP1-GFP. 51675515 can be used for the research of YAP-dependent solid tumors (including hepatocellular carcinoma, malignant mesothelioma, colorectal cancer).