Cellule staminali

LGK974 (NVP-LGK974) is a selective PORCN inhibitor that blocks Wnt signaling, used in metastatic colorectal and head/neck cancer trials. IC50: 0.4 nM.

SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.

LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .

Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.

IWP L6 (Porcn Inhibitor III) is an extremely effective Porcn inhibitor (EC50: 0.5 nM).

TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.

SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.

SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Potent oral TEAD-YAP/TAZ inhibitor-2 with 3 nM EC50; exhibits anti-proliferative and antitumor effects.

VT107 is a potent pan-TEAD autopalmitoylation inhibitor. VT-107 can be used in cancer therapy research.Cost-effective and quality-assured.

BAY 593 functions as an inhibitor of geranylgeranyltransferase-I (GGTase-I), effectively preventing the activation of Rho-GTPases and consequently inactivating YAP1/TAZ signaling pathways. It has been shown to inhibit tumor growth dose-dependently in xenograft mouse models, exhibiting IC50 values of 38.4 nM in MT-1080 cells and 564 nM in MDA-MB-231 cells, as well as in PXF 541 xenografts.

pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP/TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC₅₀ of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg/mL·min, T1/2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.

TEAD-IN-2 is a potent and bifunctional TEAD inhibitor to induce TEAD protein degradation via the ubiquitination pathway, with anticancer potential.

Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP).

VT103, an oral TEAD1 palmitoylation inhibitor, shows promise against various cancers by disrupting YAP/TAZ-TEAD interactions.

JA310 is a highly selective inhibitor of the MST3 kinase, demonstrating significant cellular potency with an EC50 value of 106 nM [1].

DMH2 is a selective BMP type I receptor (ALK2/ALK3) inhibitor. DMH2 inhibits the proliferation of lung cancer cell lines and induces cell death.

TEAD-IN-6 (Example 11-1) is a TEAD modulator that inhibits the YAP1/TAZ-TEAD interaction, and has applications in cancer research [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.

AF-2112, a TEAD inhibitor derived from Flufenamic acid, significantly diminishes the expression of CTGF, Cyr61, Axl, and NF2.