ERK Activation Inhibitor Peptide II, Cell-Permeable - Calbiochem (C15-1302-810)

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

Molecular Weight: 3146.77. Empirical Formula: C₁₃₆H₂₄₁N₅₃O₃₁S. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.