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
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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_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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