YAP

Verteporfin,a benzoporphyrin derivative monoacid ring A, is a photo-sensitizing agent for photodynamic therapy (PDT).

YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM.

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 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).

LATS-IN-1 is an inhibitor of LATS1 and LATS2 (IC 50 = 2nM for both). Lats-IN-1 inhibits core Hippo pathway kinases and activates downstream effector molecules YAP/TAZ, which translocate to the nucleus, driving expression of genes that promote cell proliferation and survival. Lats-IN-1 is primarily used to treat tissue regeneration and degenerative diseases.

Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.

K-975 is a potent and orally active inhibitor of YAP1/TAZ-TEAD protein-protein interaction.

PY-60 is a thiazole-substituted derivative with 5-phenylisoxazole as its core structure, which can potently and specifically activate the transcriptional activity of YAP (EC 50 = 1.6μM).

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.

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

VT103 is a selective TEAD1 protein palmitoylation inhibitor.

GA-017 is a selective and potent small-molecule inhibitor of LATS1 and LATS2 kinases, with IC 50 values of 4.10 ± 0.79nM for LATS1 and 3.92 ± 0.42nM for LATS2, respectively.

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.

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.

TDI-011536 is a LATS kinase inhibitor that can regulate the Hippo signaling pathway, with an IC 50 value of 0.76nM for LATS1.

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.

DC-TEADin02 is an effective inhibitor of TEAD palmitylation. It inhibits TEAD palmitylation with an IC50 value of 197 nM. DC-TEADin02 can be used for developmental, regenerative, and tissue homeostasis studies.

(R)-VT104 is the R-enantiomer of VT104. The IC50 value of (R)-VT104 for firefly luciferase is 0.1-1 μμ. VT104 is an orally active pan-TEAD deacetylase inhibitor.

TEAD-IN-3 (compound I-177) is an effective inhibitor of the TEAD transcription factor. TEAD-IN-3 can be used for research on proliferative diseases such as cancer.

VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1 and 0.52 nM for LATS2). It targets the Hippo signaling pathway and inhibits the growth of ER+ breast cancer cell lines and tumor organoids derived from patients, as well as ESR1 expression.

VT104 is an orally effective inhibitor of YAP/TAZ. It prevents the palmitoylation of endogenous TEAD1 and TEAD3 proteins. VT104 can be used in cancer research.

TT-10 (TAZ-K) is an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity.

NIBR-LTSi is a highly selective, active-site binding LATS kinase inhibitor displayed an IC 50 of 2.16µM.