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Super-TDU
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Super-TDU图片
CAS NO:1599441-71-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 5279.94
Formula C237H370N66O69S
CAS No. 1599441-71-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: N/A
Water: ~100 mg/mL (19 mM)
Ethanol: N/A
Synonyms Super-TDU; SuperTDU; Super TDU
实验参考方法
In Vitro

In vitro activity: Super-TDU (SVDDHFAKSLGDTWLQIGGSGNPKTANVPQTVPMRLRKLPDSFFKPPE) is a rationally designed inhibitor peptide that targets the YAP-TEADs interaction by mimicking the VGLL. VGLL4 is a previously identified YAP antagonist which also functions as a regulator of Wnt/β-catenin signalling. Super-TDU demonstrated therapeutic potentials for treating human cancer with YAP-activation. It reduced endogenous interaction between YAP and TEADs as shown by coIP experiment. Super-TDU inhibited cell viability and colony formation of GC cell lines MGC-803, BGC-823, and HGC27, but not MKN-45 as predicted. Moreover, the Super-TDU downregulated expression of YAP-TEADs target genes CTGF, CYR61, and CDX2. Further chromatin immunoprecipitation (ChIP) assays also showed that the Super-TDU dose-dependently reduced the amount of CTGF and CDX2 promoter cDNA ChIPed by YAP antibody. To verify the specificity of the Super-TDU, two Super-TDU mutants were created which harbor mutations that disable TEADs binding. As expected, the mutant Super-TDUs failed to interact with TEADs and inhibit cell proliferation. Thus the Super-TDU appears to have a broad but specific antitumor activity toward YAP-driven human cancers in which YAP/VGLL4 ratio should be considered as an important prognostic marker for personalized treatment.


Kinase Assay: proteins used in this study were expressed in Escherichia coli using pET28a-derived vectors and purified by affinity chromatography and size-exclusive chromatography. Diffraction data were collected at beamline BL17U, Shanghai Synchrotron Radiation Facility (SSRF) of China.


Cell Assay: Cells were transfected with the indicated plasmids of pcDNA3.1 or Flag-VGLL4 wild-type or mutant and/or HA-tagged YAP. ATP cell viability assay was used for detecting cell proliferation. ATP content was measured in accordance with the protocol of the CellTiter-Glo luminescent cell viability assay kit (Promega). Briefly, 100 μl of assay reagent was added to the wells and mixed for 2 min at room temperature. After 10 min, intracellular ATP content was measured using a luminescence multilabel counter.

In VivoSuper-TDU is a peptide mimicking this function of VGLL4 and can potently suppressed tumor growth in vitro and in vivo. It has the potential in treating gastric cancer by directly targeting YAP-TEADs, and importantly, unlike the conventional drug compound 5-FU, its antitumor activity tends to be specific toward tumors with an elevated ratio of YAP to VGLL4.
Animal modelMale nude mice (BALB/cA-nu/nu) and C57/BL6
Formulation & DosageDissolved in saline; 50 μg/kg or 500 μg/kg per day of super-TDU peptide; i.v.
References Cancer Cell. 2014 Feb 10;25(2):166-80.