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.

• Sinonimo/i: ERK Activation Inhibitor Peptide II, Cell-Permeable, MTP _TAT-G-MEK1₁₃, H- GYGRKKRRQRRR-G-MPKKKPTPIQLNP-NH₂, Erk Inhibitor V
• Formula empirica (notazione di Hill): C₁₃₆H₂₄₁N₅₃O₃₁S
• Peso molecolare: 3146.77
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: lyophilized solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Solubilità: water: 1 mg/mL
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Sequenza

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

Stato fisico

Supplied as a trifluoroacetate salt.

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable