S89387 |
TED-347 |
源叶(MedMol) | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)