产品描述: | TED-347 是一种有效的、不可逆的 the TEAD⋅Yap protein-protein interaction 的共价变构抑制剂。TED-347 可抑制 TEAD4⋅Yap1 蛋白质相互作用,其EC50值为5.9 μM |
靶点: |
TEAD4⋅Yap1(Cell-free assay):5.9 μM(EC50);YAP |
体外研究: |
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 |
细胞实验: |
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. |
参考文献: |
1. Khuchtumur Bum-Erdene, 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. |
溶解性: |
Soluble in DMSO、Ethanol |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.188 ml |
15.939 ml |
31.878 ml |
5 mM |
0.638 ml |
3.188 ml |
6.376 ml |
10 mM |
0.319 ml |
1.594 ml |
3.188 ml |
50 mM |
0.064 ml |
0.319 ml |
0.638 ml |
|
注意: |
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