YAP Inhibitor

Cardiomyocyte proliferation promoting agent-1 ((E/Z)-GA-002), which is an E/Z mixture, is a cardiomyocyte proliferation promoter. GA-002 (single E configuration) is a kinase inhibitor for LATS1 and LATS2, with its IC₅₀ values being 3.93 nM and 3.87 nM respectively. GA-002 can induce the expression of genes regulated by the Hippo pathway, inhibit the phosphorylation of YAP/TAZ, and induce the nuclear translocation of YAP.

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.

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

TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells.

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.

YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC₅₀ of 4 nM. YTP-17 shows anti-tumor efficacy.

MY-1576 is a FAK inhibitor with an IC₅₀ of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo.

(7S)-BAY-593 is the S-enantiomer of BAY-593 (HY-161573). BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.

OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC₅₀ = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research.

(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.

Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model.

(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.

Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model.

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.