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
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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
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
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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