YAP-TEAD-IN-1 TFA

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Chemical Structure| 1659305-79-9 同义名 : YAP-TEAD (Peptide 17).TFA
CAS号 : 1659305-79-9
货号 : A1211316
分子式 : C95H145ClF3N23O23S2
纯度 : 98%
分子量 : 2133.89
MDL号 : N/A
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(23.43 mM)
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.
实验方案
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
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.