yap

Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.

YAP-TEAD-IN-3 is an inhibitor of YAP TAZ-TEAD interactions with an IC50 of 9 nM for Avi-human TEAD (4217-434). YAP-TEAD-IN-3 inhibits YAP reporter gene expression (IC50 = 0.048 μM) and NCI-H2052 cell proliferation (IC50 = 0.048 μM).

AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.

YAP-TEAD-IN-2 (compound 6) is a potent inhibitor of the YAP-TEAD protein-protein interaction (PPI), with an inhibitory concentration 50 (IC50) value of 2.7 nM [1].

YAP TEAD-IN-1 (compound 4) is a potent inhibitor of YAP and TEAD, exhibiting antioxidant properties. It demonstrates antiproliferative effects on tumor cells while showing minimal cytotoxic activity towards normal human cells.

VT104 is a potent and orally active YAP TAZ inhibitor for cancer research. VT104 blocks palmitoylation of endogenous TEAD1 and TEAD3 proteins.

YAP TAZ inhibitor-1 is a YAP TAZ inhibitor (IC50 <0.100 μΜ) for the study of abnormal immune function and cancer.

YAP-TEAD-IN-1 acetate is an effective and competitive inhibitor of YAP–TEAD interaction with an IC50 of 25 nM.

YAP TAZ inhibitor-2 is a potent, orally active TEAD-YAP TAZ inhibitor with an EC50 value of 3 nM, demonstrating anti-proliferative and antitumor activity [1].

YAP TAZ Inhibitor-4 (Compound 45) acts as an inhibitor of YAP TAZ, exhibiting inhibitory activity on TEAD transcriptional activation by preventing the interaction between YAP or TAZ and TEAD.

YAP TAZ-TEAD-IN-2 (Compound 51) is a YAP TAZ-TEAD inhibitor that disrupts the interaction between YAP TAZ and TEAD. It inhibits the transcriptional activity of TEAD with an IC50 of 1.2 nM. Additionally, YAP TAZ-TEAD-IN-2 suppresses the expression of target genes (Cyr61, CTGF, AXL, and Survivin) and the proliferation of breast cancer cells.

MY-1076 is a potent YAP inhibitor with antigastric cancer activity.MY-1076 dose-dependently induced G2 M phase block, induced YAP degradation and apoptosis, and inhibited microtubule protein polymerization.MY-1076 inhibited the proliferation of MGC-803, SGC-7901, HCT-116, and KYSE450 cells.

PROTAC YAP degrader-1, a targeted proteolysis promoting chimeric molecule, both degrades the YAP protein and inhibits its nuclear localization. This compound is formulated with Demethyl-NSC682769 as the target protein ligand, and utilizes (R,S,R)-AHPC-PEG2-C2-boc, which is the E3 ubiquitin ligase ligand + Linker conjugate. The linker incorporated in the design is Acid-PEG2-C2-Boc.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5 0.57 0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

YAP-TEAD-IN-1 TFA, a competitive inhibitor of the YAP–TEAD interaction (IC50: 25 nM), exhibits higher binding affinity to TEAD1 (Kd: 15 nM) compared to YAP (50-171) (Kd: 40 nM).

Compound 24, also known as YAP TAZ inhibitor-3, effectively inhibits YAP TAZ. It displays significant inhibitory activity against firefly luciferase, demonstrating an IC 50 value of less than 0.1 μM [1].

YAP-TEAD-IN-1 is a competitive inhibitor of YAP–TEAD interaction (IC50: 25 nM) and exhibits higher binding affinity to TEAD1 (Kd: 15 nM) compared to YAP (50-171) (Kd: 40 nM).

4-Methylayapin is a useful organic compound for research related to life sciences. The catalog number is T7038 and the CAS number is 15071-04-2.

2,3,5,6-Tetramethoxyaporphine, a benzyl isoquinoline alkaloid with antitussive properties, can be extracted from Glaucium flavum Cr. (Family Papaveraceae) [1] [2].

6-Hydroxyapigenin 3,6-diglucoside is a natural product that can be used in related research in the field of life sciences. Its product number is TN8701.

2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.

3,6-Dimethoxyapigenin is a natural product of Dodonaea, Sapindaceae. The catalog number is TN2907 and the CAS number is 22697-65-0. 3,6-Dimethoxyapigenin can be used as a reference standard.

(−)-N-Hydroxyapiosporamide (NHAP), an alkaloid, serves as an NF-κB inhibitor and demonstrates significant antitumor activity both in vitro and in vivo, with potential applications in colorectal cancer (CRC) research [1].