|2-氯-1-(2-((3-(三氟甲基)苯基)氨基)苯基)乙酮|CsnPharm

CAS No.: 2378626-29-8

TED-347 Catalog No. CSN26165

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

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400-920-2911

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技术信息

生物活性

描述Yap1, which binds tightly to TEAD4 via a large flat interface, promotes tumor progression and metastasis through its TEAD-interaction domain. TED-347 is a potent and irreversible covalent allosteric inhibitor of the TEAD⋅Yap interaction. Following 24 hr incubation of TEAD4 with TED-347 at 4 ℃, the compound inhibited the TEAD⋅Yap protein-protein interaction by 53% with an apparent EC₅₀ of 5.9 μM. TED-347 was found to inhibit the protein-protein interaction in a time-dependent manner (0.5, 6, 24, and 48 hr), and it reached maximum inhibition of 80% at 48 hr. In HEK-293 cells transfected with a TEAD reporter, TED-347 (5 μM; 48 hr) resulted in over 70% reduction in reporter activity, whereas cells treated with 10 μM of TED-347 showed a complete loss of reporter activity, suggesting TED-347 inhibits TEAD transcriptional activity and protein-protein interactions in cell culture. Moreover, TED-347 (10 μM) inhibited GBM43 cancer cell viability by 30%^[2].
作用机制TED-347 forms a covalent bond with a conserved Cys-367 located within the unique deep hydrophobic palmitate-binding pocket of TEADs^[2].
参考文献

[1] Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction
[2] Bum-Erdene K, et al. Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction. Cell Chem Biol. 2019 Mar 21;26(3):378-389.e13

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1877 mL
- 15.9387 mL
- 31.8774 mL
- 5 mM
- 0.6375 mL
- 3.1877 mL
- 6.3755 mL
- 10 mM
- 0.3188 mL
- 1.5939 mL
- 3.1877 mL

技术信息

CAS号

2378626-29-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H11ClF3NO

运输

蓝冰

分子量

313.70

别名

溶解度

DMSO	69.0 mg/mL (220.0 mM)
Water	Insoluble
Ethanol	25.0 mg/mL (79.7 mM)

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