TED-347

製品コードS8951 バッチS895101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₅H₁₁ClF₃NO

分子量

313.70

CAS No.

2378626-29-8

Solubility (25°C)*

体外

DMSO

69 mg/mL (219.95 mM)

Ethanol

25 mg/mL (79.69 mM)

Water

˂1 mg/mL

体内（毎回新しく調製した物を用意してください）

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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK-293 cells, GBM43 cells
	濃度	0.5 µM, 1.0 µM, 5.0 µM, 10 µM, 25 µM
	反応時間	48 h
	実験の流れ	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.

参考

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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