|(S)-4-((S)-1-((S)-1-((S)-2-((3S,6S,9S,12R,18S,21S,24S,27S,30S,35AS)-18-((S)-2-((S)-1-((S)-2-乙酰氨基-3-甲基丁酰基)吡咯烷-2-甲酰胺基)-3-(3-氯苯基)丙酰胺基)-27-(4-氨基丁基)-9-苄基-30-丁基-24-(3-胍基丙基)-6-(羟甲基)-21-异丁基-3-甲基-1,4,7,10,19,22,25,28,31-九氧代三十二氢-1H-吡咯烷[2,1-p][1,2,5,8,11,14,17,20,23,26,29]dithianonaazacyclotritriacontine-12-甲酰胺基)-6-氨基己酰基)吡咯烷-2-羰基)吡咯烷-2-甲酰胺)-5-氨基-5-氧代戊酸2,2,2-三氟乙酸 (1:x)|CsnPharm

CAS No.: 1659305-79-9

YAP-TEAD-IN-1 TFA Catalog No. CSN25239

Synonyms: 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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400-920-2911

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tech@csnpharm.cn

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技术信息

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 K_d = 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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.4686 mL
- 2.3431 mL
- 4.6863 mL
- 5 mM
- 0.0937 mL
- 0.4686 mL
- 0.9373 mL
- 10 mM
- 0.0469 mL
- 0.2343 mL
- 0.4686 mL

技术信息

CAS号	1659305-79-9	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C95H145ClF3N23O23S2	运输	蓝冰
分子量	2133.89	别名	Peptide 17 TFA

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YAP-TEAD-IN-1 TFA Catalog No. CSN25239

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