Chemical Name: α-[Amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitrile
Biological ActivitySL 327 is a selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The MAPK/ERK cascade targets both Elk-1 and cAMP response element-binding protein to control long-term potentiation-dependent gene expression in the dentate gyrus in vivo.
Davis et al.
Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy.
Scherle et al.
Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis.
Wang et al.
The MAPK cascade is required for mammalian associative learning.
Atkins et al.
Nature Neurosci., 1998;1:602
Citations for SL 327
The citations listed below are publications that use Tocris products. Selected citations for SL 327 include:
20 Citations: Showing 1 - 10
The Protective Effect of Ins. on Rat Cortical Neurons in Oxidative Stress and Its Dependence on the Modulation of Akt, GSK-3beta, ERK1/2, and AMPK Activities.
Authors: Zakharova Et al.
Int J Mol Sci 2019;20
Negative regulation of ERK1/2 by PI3K is required for the protective effects of Pyropia yezoensis peptide against perfluorooctane sulfonate-induced endoplasmic reticulum stress.
Authors: Oh Et al.
Mol Med Rep 2017;15:2583
Cell type-dependent Erk-Akt pathway crosstalk regulates the proliferation of fetal neural progenitor cells
Authors: Rhim Et al.
Scientific Reports 2016;6:26547
Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
Authors: Liddell Et al.
J Neuroinflammation 2016;13:49
Targeting β-arrestin2 in the treatment of L-DOPA-induced dyskinesia in Parkinson's disease.
Authors: Urs Et al.
J Biol Chem 2015;112:E2517
mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
Authors: Kubota Et al.
PLoS One 2014;9:e106316
G Protein and β-arrestin signaling bias at the ghrelin receptor.
Authors: Evron Et al.
J Biol Chem 2014;289:33442
Mechanism and treatment for learning and memory deficits in mouse models of Noonan syndrome.
Authors: Lee Et al.
Nat Neurosci 2014;17:1736
Spaced training rescues memory and ERK1/2 signaling in fragile X syndrome model mice.
Authors: Seese Et al.
Proc Natl Acad Sci U S A 2014;111:16907
Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
Authors: Keasey Et al.
Cell Commun Signal 2013;11:35
A DA D1 receptor-dependent β-arrestin signaling complex potentially regulates morphine-induced psychomotor activation but not reward in mice.
Authors: Urs Et al.
Erk1/2 inhibit synaptic vesicle exocytosis through L-type calcium channels.
Authors: Subramanian and Morozov
J Neurosci 2011;31:4755
A metabolic perturbation by U0126 identifies a role for glutamine in resveratrol-induced cell death.
Authors: Freeman Et al.
Cancer Biol Ther 2011;12:966
Hypersensitivity to mGluR5 and ERK1/2 leads to excessive protein synthesis in the hippocampus of a mouse model of fragile X syndrome.
Authors: Osterweil Et al.
J Neurosci 2010;30:15616
Genetic targeting of ERK1 suggests a predominant role for ERK2 in murine pain models.
Authors: Alter Et al.
J Neurosci 2010;30:11537
Heme oxygenase activity and hemoglobin neurotoxicity are attenuated by inhibitors of the MEK/ERK pathway.
Authors: Chen-Roetling Et al.
Increased operant responding for ethanol in male C57BL/6J mice: specific regulation by the ERK1/2, but not JNK, MAP kinase pathway.
Authors: Faccidomo Et al.
Psychopharmacology (Berl) 2009;204:135
Effects of opiate drugs on Fas-associated protein with death domain (FADD) and effector caspases in the rat brain: regulation by the ERK1/2 MAP kinase pathway.
Authors: García-Fuster Et al.
Proc Natl Acad Sci U S A 2007;32:399
Paradoxical striatal cellular signaling responses to psychostimulants in hyperactive mice.
Authors: Beaulieu Et al.
An Akt/beta-arrestin 2/PP2A signaling complex mediates DArgic neurotransmission and behavior.
Authors: Beaulieu Et al.
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