TED-347

Catalog No.S8951 Batch:S895101

Technical Data

Formula

C₁₅H₁₁ClF₃NO

Molecular Weight

313.70

CAS No.

2378626-29-8

Solubility (25°C)*

In vitro

DMSO

69 mg/mL (219.95 mM)

Ethanol

25 mg/mL (79.69 mM)

Water

˂1 mg/mL

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM.

Targets

TEAD4⋅Yap1 ^[1]
(Cell-free assay)

5.9 μM(EC50)

In vitro

TED-347 is found to inhibit the protein-protein interaction in a time-dependent manner. TED-347 is shown to functionally disrupt the TEAD·Yap1 interaction in cells and to reduce the viability of patient-derived glioblastoma cell lines.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HEK-293 cells, GBM43 cells Concentrations 0.5 µM, 1.0 µM, 5.0 µM, 10 µM, 25 µM Incubation Time 48 h Method HEK-293 or GBM43 cells are plated at 2.43104 cells/well in a 96-well microplate and are transfected after 24 hr with the a pGL3.1 reporter containing the CTGF promoter and a plasmid encoding TK-Renilla luciferase in combination with control vectors or vectors that express Yap1 and TEAD4. After 48 hr, cells are treated with 0.5, 1.0, 5.0 or 10 µM of TED-347 for another 48 hr.

Cell Assay:^{^[1]}

Cell lines
HEK-293 cells, GBM43 cells
Concentrations
0.5 µM, 1.0 µM, 5.0 µM, 10 µM, 25 µM
Incubation Time
48 h
Method
HEK-293 or GBM43 cells are plated at 2.43104 cells/well in a 96-well microplate and are transfected after 24 hr with the a pGL3.1 reporter containing the CTGF promoter and a plasmid encoding TK-Renilla luciferase in combination with control vectors or vectors that express Yap1 and TEAD4. After 48 hr, cells are treated with 0.5, 1.0, 5.0 or 10 µM of TED-347 for another 48 hr.

References

[1] Khuchtumur Bum-Erdene, et al. Cell Chem Biol. 2019 Mar 21;26(3):378-389.e13.

Selleck's TED-347 has been cited by 4 publications

Releasing YAP dysfunction-caused replicative toxicity rejuvenates mesenchymal stem cells [ Aging Cell, 2023, e13913.]	PubMed: 37340571
Transcriptional and epigenomic profiling identifies YAP signaling as a key regulator of intestinal epithelium maturation [ Sci Adv, 2023, 9(28):eadf9460]	PubMed: 37436997
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106 [ J Med Chem, 2022, 65(13):9206-9229]	PubMed: 35763499
Upregulated YAP promotes oncogenic CTNNB1 expression contributing to molecular pathology of hepatoblastoma [ Pediatr Blood Cancer, 2022, e29705]	PubMed: 35404538

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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