货号:A1211316 同义名: YAP-TEAD (Peptide 17).TFA
YAP-TEAD Inhibitor 1 is an inhibitor of this YAP-TEAD protein-protein interaction which has potential usage in treatment of YAP-involved cancers with IC50 of 25nM.
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描述 | As the downstream effectors, Yes-associated protein (YAP)-transcriptional enhancer activation domain family member (TEAD) association is essential for YAP-driven oncogenic activity, while TEAD is largely dispensable for normal tissue growth [3]. YAP-like peptides YAP-TEAD Inhibitor 1 TFA (Peptide 17) which can occupy the interface 3 on TEAD is a potent cyclic peptide inhibitor of the YAP-TEAD interaction with an IC50 of 25 nM, and the binding affinity of this 17mer peptide to TEAD1 is Kd = 15 nM. Peptide 17 significantly improves the potency in disrupting YAP-TEAD interaction in vitro [4]. |
作用机制 | The meta-Cl-phenyl ring of Phe(3-Cl) in peptide 17 forms extensive hydrophobic interactions with Val406, Ile262, and the side chain of Lys265 of TEAD1. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.47mL 0.09mL 0.05mL |
2.34mL 0.47mL 0.23mL |
4.69mL 0.94mL 0.47mL |
CAS号 | 1659305-79-9 |
分子式 | C95H145ClF3N23O23S2 |
分子量 | 2133.886 |
别名 | YAP-TEAD (Peptide 17).TFA |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
H2O: 50 mg/mL(23.43 mM) |
动物实验配方 |