328000

ERK Activation Inhibitor Peptide I, Cell-Permeable

The ERK Activation Inhibitor Peptide I, 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 I, Cell-Permeable, Ste-MEK1₁₃, Ste-MPKKKPTPIQLNP-NH₂, Erk Inhibitor IV
• Empirical Formula (Hill Notation): C₈₆H₁₅₃N₁₉O₁₇S
• Molecular Weight: 1757.32
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: lyophilized solid
• potency: 2.5 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 1 mg/mL; DMSO: 5 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A cell-permeable and reversible stearated 13-amino acid peptide corresponding to the N-terminus of MEK1 (MAPKK) that 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 = 2.5 µM). Potently blocks ERK activation in PMA-stimulated NIH 3T3 cells and NGF-treated PC12 cells (IC₅₀ = 13 µM). Does not affect the activation of JNKs or p38.

A cell-permeable, reversible, and stearated, 13-amino acid peptide corresponding to the N-terminus of MAPK/ERK kinase (MEK). 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 = 2.5 µM). Shown to block ERK activity in PMA-stimulated NIH3T3 cells and NGF-treated PC12 cells (IC₅₀ = 13 µM). Does not affect the activation of either JNKs or p38 MAP kinase.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

Ste-Met-Pro-Lys-Lys-Lys-Pro-Thr-Pro-Ile-Gln-Leu-Asn-Pro-NH₂ (Ste = stearated)

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 Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable