1. Peptides
  2. TAT-DEF-Elk-1

TAT-DEF-Elk-1 (Synonyms: TDE)

Cat. No.: HY-P2262
Handling Instructions

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.

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TAT-DEF-Elk-1 Chemical Structure

TAT-DEF-Elk-1 Chemical Structure

CAS No. : 1220751-16-5

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Description

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]

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].

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.
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].

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.
Molecular Weight

3561.07

Formula

C₁₅₅H₂₅₉N₅₇O₄₀

CAS No.

1220751-16-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

TAT-DEF-Elk-1TDEOthersDepressionhippocampalantidepressantPrimarystriatalneuronneuronalplasticityInhibitorinhibitorinhibit

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