Pep2m, myristoylated TFA

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).

Product information

Molecular Weight: 1497.81

Formula: C65H119F3N18O16S

Synonym:

Myr-Pep2m TFA

Chemical Name: (2S, 5S, 8S, 11S, 14S, 17S, 20S, 23S, 26S, 29S)-8-(2-amino-2-oxoethyl)-2-(3-amino-3-oxopropyl)-11, 20, 29-tris(4-aminobutyl)-26-(3-(diaminomethyleneamino)propyl)-17-isopropyl-5, 14-dimethyl-23-(2-(methylthio)ethyl)-4, 7, 10, 13, 16, 19, 22, 25, 28, 31-decaoxo-3, 6, 9, 12, 15, 18, 21, 24, 27, 30-decaazatetratetracontan-1-oic acid compound with 2, 2, 2-trifluoroacetic acid (1:1)

Smiles: CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)CCCCCCCCCCCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(O)=O.OC(=O)C(F)(F)F

InChiKey: LKKZFINUWDZEHG-HVXFLXQCSA-N

InChi: InChI=1S/C63H118N18O14S.C2HF3O2/c1-7-8-9-10-11-12-13-14-15-16-17-29-51(84)74-42(25-18-21-33-64)55(87)77-45(28-24-36-71-63(69)70)56(88)78-46(32-37-96-6)58(90)76-44(27-20-23-35-66)59(91)81-52(39(2)3)61(93)73-41(5)53(85)75-43(26-19-22-34-65)57(89)80-48(38-50(68)83)60(92)72-40(4)54(86)79-47(62(94)95)30-31-49(67)82;3-2(4,5)1(6)7/h39-48,52H,7-38,64-66H2,1-6H3,(H2,67,82)(H2,68,83)(H,72,92)(H,73,93)(H,74,84)(H,75,85)(H,76,90)(H,77,87)(H,78,88)(H,79,86)(H,80,89)(H,81,91)(H,94,95)(H4,69,70,71);(H,6,7)/t40-,41-,42-,43-,44-,45-,46-,47-,48-,52-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Pep2m, myristoylated TFA (10 μM) blocks PKMζ-mediated AMPA receptor (AMPAR) potentiation. 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. 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.

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.

References:

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.

Products are for research use only. Not for human use.