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

发表于由

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

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

TAT-DEF-Elk-1 TFA Chemical Structure

规格 价格 是否有货
1 mg ￥1500 询问价格 货期
5 mg ￥4500 询问价格 货期
10 mg ￥7500 询问价格 货期

* Please select Quantity before adding items.

生物活性

TAT-DEF-Elk-1 TFA (TDE TFA) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 TFA blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 TFA 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 TFA (5 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 TFA (5-10 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[2]

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[2]

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

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: 1 mg/kg
Administration: Intraperitoneal injection; daily; 14 days
Result: Reversed social-defeat induced decrease of hippocampal Bdnf expression by repeated TDE administration.

分子量

3675.09

Formula

C157H260N57F3O42
Sequence

Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Ser-Pro-Ala-Lys-Leu-Ser-Phe-Gln-Phe-Pro-Ser-Ser-Gly-Ser-Ala-Gln-Val-His-Ile
Sequence Shortening

GRKKRRQRRRPPSPAKLSFQFPSSGSAQVHI
运输条件

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

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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.

    [2]. Apazoglou K, et al. Antidepressive effects of targeting ELK-1 signal transduction.Nat Med. 2018 May;24(5):591-597.