| 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].
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| Related Catalog |
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| Target |
IC50: Elk-1[1]
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| 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.
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| 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.
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| References |
[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.
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