328005

ERK Activation Inhibitor Peptide II, Cell-Permeable

The ERK Activation Inhibitor Peptide II, Cell-Permeable controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): ERK Activation Inhibitor Peptide II, Cell-Permeable, MTP _TAT-G-MEK1₁₃, H- GYGRKKRRQRRR-G-MPKKKPTPIQLNP-NH₂, Erk Inhibitor V
• Empirical Formula (Hill Notation): C₁₃₆H₂₄₁N₅₃O₃₁S
• Molecular Weight: 3146.77
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• solubility: water: 1 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A cell-permeable and reversible 13-amino acid peptide corresponding to the N-terminus of MAPK/ERK kinase (MEK or MAPKK) that is fused to the HIV-TAT membrane translocation peptide (MTP) sequence via a glycine linker. Acts as a specific inhibitor of ERK activation by MEK1 and the downstream transcriptional activity of ELK1. Selectively binds to ERK2 and prevents its interaction with MEK (IC₅₀ = 210 nM in vitro). Potently blocks ERK in PMA-stimulated NIH3T3 cells and NGF-treated PC12 cells (IC₅₀ = 29 µM). Does not inhibit the activation of c-jun N-terminal kinases (JNKs) or p38 MAP kinase.

A cell-permeable and reversible 13-amino acid peptide corresponding to the N-terminus of MEK1 (MAPKK) that is fused to the HIV-TAT membrane translocating peptide (MTP) sequence via a glycine linker. Acts as a specific inhibitor of ERK activation and blocks the transcriptional activity of Elk1. Selectively binds to ERK2 and prevents its interaction with MEK (IC₅₀ = 210 nM). Potently blocks ERK activation in PMA-stimulated NIH 3T3 cells and NGF-treated PC12 cells (IC₅₀ = 29 µM). Does not affect the activation of JNKs or p38.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 210 nM against MEK; 29 µM in blocking ERK activation in PMA-stimulated NIH 3T3 cells and NGF-treated PC12 cells

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

H-Gly-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Met-Pro-Lys-Lys-Lys-Pro-Thr-Pro-Ile-Gln-Leu-Asn-Pro-NH₂

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kelemen, B.R., et al. 2002. J. Biol. Chem.277, 8741.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable