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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C136H241N53O31S
Molecular Weight:
3146.77
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
lyophilized solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

Key Documents

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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

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Martha M Monick et al.
Journal of immunology (Baltimore, Md. : 1950), 177(3), 1636-1645 (2006-07-20)
Human alveolar macrophages, central to immune responses in the lung, are unique in that they have an extended life span in contrast to precursor monocytes. We have shown previously that the ERK MAPK (ERK) pathway is constitutively active in human

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