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TED-347

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Chemical Structure| 2378626-29-8 同义名 : -
CAS号 : 2378626-29-8
货号 : A1281058
分子式 : C15H11ClF3NO
纯度 : 99%+
分子量 : 313.702
MDL号 : MFCD32689460
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(334.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.94mL

3.19mL

1.59mL

31.88mL

6.38mL

3.19mL
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