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YAP-TEAD-IN-1 TFA {[allProObj[0].p_purity_real_show]}

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.

YAP-TEAD-IN-1 TFA 化学结构 CAS号:1659305-79-9
YAP-TEAD-IN-1 TFA 化学结构
CAS号:1659305-79-9
YAP-TEAD-IN-1 TFA 3D分子结构
CAS号:1659305-79-9
YAP-TEAD-IN-1 TFA 化学结构 CAS号:1659305-79-9
YAP-TEAD-IN-1 TFA 3D分子结构 CAS号:1659305-79-9
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YAP-TEAD-IN-1 TFA 纯度/质量文件 产品仅供科研

货号:A1211316 标准纯度: {[allProObj[0].p_purity_real_show]}
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YAP-TEAD-IN-1 TFA 生物活性

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.

YAP-TEAD-IN-1 TFA 参考文献

[1]Zhang Z, Lin Z, Zhou Z, et al. Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction. ACS Med Chem Lett. 2014;5(9):993-8

[2]Zhou Z, Hu T, Xu Z, et al. Targeting Hippo pathway by specific interruption of YAP-TEAD interaction using cyclic YAP-like peptides. FASEB J. 2015;29(2):724-32

[3]Zhou Z. Targeting Hippo pathway by specific interruption of YAP-TEAD interaction using cyclic YAP-like peptides. FASEB J. 2015 Feb;29(2):724-32. doi: 10.1096/fj.14-262980. Epub 2014 Nov 10. Erratum in: FASEB J. 2017 Apr;31(4):1767.

[4]Zhang Z. Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction. ACS Med Chem Lett. 2014 Jul 14;5(9):993-8. doi: 10.1021/ml500160m.

YAP-TEAD-IN-1 TFA 实验方案

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

YAP-TEAD-IN-1 TFA 技术信息

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
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