Cellule staminali

TM2 TEAD inhibitor, a robust and reversible inhibitor of the TEA domain transcription factor, presents dual inhibitory concentrations (IC50) of 38 nM for TEAD4

TGFβ-IN-5 (WAY-641966) is a potent TGFβ inhibitor with anti-prion activity for the study of fibroproliferative diseases associated with TGF-β signaling.

GNE-7883 is an inhibitor targeting TEAD transcription factor, inhibits cell proliferation and suppresses YAP/TAZ activation, and can be used to study YAP/TAZ-dependent tumors.

(+)-ITD-1 is an inhibitor of TGF-β, effectively inhibiting TGF-β2 with an IC50 of 0.46 μM. It promotes the degradation of the TGF-β type II receptor (TGFBR2) and the differentiation of cardiomyocytes. Additionally, it suppresses the formation of the mesoderm during the early differentiation of mouse embryonic stem cells (mESCs).

LATS1/2-IN-1 is a potent and selective inhibitor of LATS1 and LATS2. In the r33P functional assay, it demonstrates strong inhibitory activity with IC50 values of 4.4 nM for LATS1 and 5.5 nM for LATS2. The NanoBRET assay determined the cellular IC50 values as 136 nM for LATS1 and 36.0 nM for LATS2. This compound reduces YAP1 phosphorylation levels in mouse liver. Additionally, LATS1/2-IN-1 shows wound healing activity in HT-1080 scratch assays and in vivo SKH1 mouse punch biopsy models. It is applicable for research into regenerative medicine-related conditions, such as wound healing.

TEAD-IN-23 (Compound 22) is a potent pan-TEAD inhibitor with an IC50 of 10 nM. It exhibits strong antiproliferative activity against NCI-H226 and MSTO-211H cell lines. In the MSTO-211H xenograft tumor model, TEAD-IN-23 causes complete tumor regression. This compound is suitable for research on mesothelioma and hepatocellular carcinoma.

YAP/TEAD-IN-2 (Compound T-1) is an inhibitor of YAP/TEAD. This compound suppresses luciferase activity driven by YAP/TEAD in 293T cells and exhibits strong antiproliferative effects on human pleural mesothelioma NCI-H226 cells. YAP/TEAD-IN-2 is applicable for studying diseases associated with disruptions in the Hippo pathway, particularly cancer.

(Rac)-SAG, an isoform of SAG, is a potent Smoothened (Smo) receptor agonist (EC₅₀ = 3 nM; Kd = 59 nM) that activates the Hedgehog signaling pathway and counteracts Cyclopamine's inhibition of Smo [1] [2] [3].

Kartogenin (KGN) sodium acts as an inducer of chondrogenic tissue formation (EC 50: 100 nM). It promotes chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and modulating the CBFβ-RUNX1 transcriptional program. Additionally, Kartogenin sodium aids tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. It is extensively utilized in cell-free therapies for cartilage regeneration and protection, tendon-bone healing, wound healing, and limb development. The compound is also vital for cartilage repair, coordinating limb development, and osteoarthritis (OA) research [1] [2] [3] [4].

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) with an IC50 of 4.1 μM. It inhibits TGFβ signaling by promoting protein degradation of TGFβ RII. Additionally, TGFβRI-IN-7 can block the transition from endothelial to mesenchymal states and inhibit cell migration, making it useful for cancer research.

Ontunisertib is a selective, orally available, gastrointestinal-restricted small-molecule inhibitor of TGFβ receptor I (ALK5/TGFβR1) that blocks the pro-fibrotic TGF-β/ALK5 signaling pathway, with a cellular ALK5 inhibition IC₅₀ ≤100 nM. By limiting systemic exposure and increasing local gastrointestinal drug exposure, Ontunisertib is primarily used for research on fibrostenotic Crohn's disease and intestinal fibrosis-related studies. Ontunisertib can also be used to study the mechanisms of fibrosis and inflammatory regulation mediated by TGF-β/ALK5 signaling.

MYF-03-176 is an orally active TEAD1/3/4 inhibitor with IC₅₀ values of 47/32/71 nM. inhibits TEAD transcriptional activity and cancer cell growth, antitumour.

TEAD-IN-20 is a TEAD inhibitor with IC₅₀ values of 0.021 μM in TEAD4 FRET and 0.044 μM in TEAD4 MCF7-Tead cell lines. It has potential applications in cancer research.

TEAD-IN-1 (Compound 2) is an effective inhibitor of TEAD auto-palmitoylation with an IC₅₀ of 603 nM. It enhances the interaction between TEAD and VGLL4, while diminishing the interaction between YAP and TEAD. TEAD-IN-1 is applicable for cancer research.

THRX-144644 is a lung-selective ALK5 inhibitor with a biochemical IC50 value of 0.14 nM, can inhibit ALK5 in BEAS-2B cells, and targets the lung after inhaled administration in rats.

CDD-1431 is a highly selective BMPR2 kinase inhibitor with a Kiapp of 20.6 nM. It inhibits BRE reporter gene activity, exhibiting an IC50 of 4.87 μM. BMPs regulate cellular processes across various tissue types such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.

YAP/TAZ inhibitor-3 (Compound 24) is a YAP/TAZ inhibitor applicable for relevant research within the life sciences field.

TEAD-IN-10 (compound 15), a covalent inhibitor, exhibits selective and potent inhibitory activity against TEAD1 (IC 50 =14 nM), TEAD2 (IC 50 =179 nM), and TEAD3 (IC 50 =4 nM). This compound is utilized in cancer research [1].

TEAD-IN-22 (compound I) is a TEAD inhibitor with potential applications in cancer and fibrosis research.

TEAD-IN-24 (Example 65) is a TEAD inhibitor with anticancer activity against non-small cell lung cancer.