TAT-DEF-Elk-1(Synonyms: TDE)

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TAT-DEF-Elk-1;(Synonyms: TDE)

TAT-DEF-Elk-1 (TDE) 是 Elk-1 的一种可穿透细胞的肽抑制剂，通过模仿和特异性干扰 Elk-1 的 DEF 结构域来实现抑制。TAT-DEF-Elk-1 阻止 Elk-1 磷酸化并防止 Elk-1 核易位，且不会干扰 ERK 或 MSK1 活化。TAT-DEF-Elk-1 是分析神经元可塑性发展过程中 Elk-1 在此过程中的作用的有用工具。

TAT-DEF-Elk-1amp;;(Synonyms: TDE)

TAT-DEF-Elk-1 Chemical Structure

CAS No. : 1220751-16-5

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生物活性

TAT-DEF-Elk-1 (TDE) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity[1].
IC50 Target

IC50: Elk-1[1]
体外研究
(In Vitro)

Elk-1 phosphorylation on Ser383/389 has a dual function and triggers both Elk-1 nuclear translocation and SRE-dependent gene expression[1].
TAT-DEF-Elk-1 (5-10 μM; 1 hour) specifically inhibits glutamate-induced elk-1 activation and does not interfer with ERK, MSK-1, or CREB phosphorylation[1].
TAT-DEF-Elk-1 (5 μM; 2 hour) treatment shows a significant inhibition of c-Fos, Zif268 and JunB, but has no effects on c-Jun expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Neurons
Concentration: 5 μM; 10 μM
Incubation Time: 1 hour
Result: Decreased Elk-1 expression and had no effects on ERK, MSK-1, or CREB phosphorylation.

RT-PCR[1]

Cell Line: Primary striatal neurons
Concentration: 5 μM
Incubation Time: 2 hour
Result: Decreased c-Fos, Zif268 and JunB mRNA level but did not effect c-Jun.

体内研究
(In Vivo)

TAT-DEF-Elk-1 (intraperitoneal injection; 1mg/kg; daily; 14 days) reflects antidepressant efficacy in mice, it decreases immobility similar to the reference antidepressants fluoxetine and desipramine (DMI)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl6 mice (3-6 months old males) are subjected to social defeat stress[2]
Dosage: 1mg/kg;
Administration: Intraperitoneal injection; daily; 14 days
Result: Reversed social-defeat induced decrease of hippocampal Bdnf expression by repeated TDE administration.

分子量

3561.07

Formula

C155H259N57O40
CAS 号

1220751-16-5
Sequence Shortening

GRKKRRQRRRPPSPAKLSFQFPSSGSAQVHI
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lavaur J, et al. A TAT-DEF-Elk-1 peptide regulates the cytonuclear trafficking of Elk-1 and controls cytoskeleton dynamics.J Neurosci. 2007 Dec 26;27(52):14448-58.