| Bioactivity | Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC)[1][2]. | ||||||
| Target | NSF/GluR2 interactions | ||||||
| Invitro | Pep2m, myristoylated TFA (10 μM) blocks PKMζ-mediated AMPA receptor (AMPAR) potentiation[1].Pep2m, myristoylated TFA does not block the increase of PKMζ in the hippocampal slices during long-term potentiation (LTP) maintenance, indicating that blocking NSF/GluR2 interactions do not prevent the induction of PKMζ synthesis[1].Pep2m, myristoylated TFA blocks NSF/GluR2-mediated AMPAR trafficking, and reverses persistent potentiation at both the strongly stimulates synapses and the weakly stimulats synapses that underwent synaptic tagging and capture[1]. | ||||||
| In Vivo | Pep2m, myristoylated TFA (10 µg/20 µL) results in an increase in paw withdrawal thresholds (PWTs) on nociceptive responses in the formalin test[2]. Animal Model: | ||||||
| Name | Pep2m, myristoylated TFA | ||||||
| Shortening | {Myr}-KRMKVAKNAQ | ||||||
| Formula | C65H119F3N18O16S | ||||||
| Molar Mass | 1497.83 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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| Reference | [1]. Yudong Yao, et al. PKMζ Maintains Late Long-Term Potentiation by N-Ethylmaleimide-Sensitive Factor/GluR2-Dependent Trafficking of Postsynaptic AMPA Receptors. J Neurosci. 2008 Jul 30; 28(31): 7820-7827. [2]. Nicole C George, et al. Sex differences in the contributions of spinal atypical PKCs and downstream targets to the maintenance of nociceptive sensitization. Mol Pain. 2019; 15: 1744806919840582. |