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Biological Activity for SL 327
SL 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.
Technical Data for SL 327
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SL 327
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for SL 327
The following data is based on the product molecular weight 335.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.98 mL||14.91 mL||29.82 mL|
|5 mM||0.6 mL||2.98 mL||5.96 mL|
|10 mM||0.3 mL||1.49 mL||2.98 mL|
|50 mM||0.06 mL||0.3 mL||0.6 mL|
References for SL 327
References are publications that support the biological activity of the product.
Davis et al (2000) 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. J.Neurosci. 20 4563 PMID: 10844026
Scherle et al (2000) Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy. J.Biol.Chem. 275 37086 PMID: 10969080
Wang et al (2003) Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis. J.Pharmacol.Exp.Ther. 304 172 PMID: 12490588
Atkins et al (1998) The MAPK cascade is required for mammalian associative learning. Nature Neurosci. 1 602 PMID: 10196568
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Keywords: SL 327, SL 327 supplier, Selective, inhibitors, inhibits, MEK1, MEK2, brain, penetrant, Mitogen-Activated, Protein, Kinase, MEK, Kinases, SL327, 1969, Tocris Bioscience
20 Citations for SL 327
Citations are publications that use Tocris products. Selected citations for SL 327 include:
Alter et al (2010) Genetic targeting of ERK1 suggests a predominant role for ERK2 in murine pain models. J Neurosci 30 11537 PMID: 20739576
Liddell et al (2016) Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes. J Neuroinflammation 13 49 PMID: 26920699
Rhim et al (2016) Cell type-dependent Erk-Akt pathway crosstalk regulates the proliferation of fetal neural progenitor cells Scientific Reports 6 26547 PMID: 27211495
Urs et al (2015) Targeting β-arrestin2 in the treatment of L-DOPA-induced dyskinesia in Parkinson's disease. J Biol Chem 112 E2517 PMID: 25918399
García-Fuster et al (2007) 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. Proc Natl Acad Sci U S A 32 399 PMID: 16482086
Beaulieu et al (2006) Paradoxical striatal cellular signaling responses to psychostimulants in hyperactive mice. Neuropsychopharmacology 281 32072 PMID: 16954211
Zakharova et al (2019) 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. Int J Mol Sci 20 PMID: 31362343
Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35 PMID: 23693126
Faccidomo et al (2009) Increased operant responding for ethanol in male C57BL/6J mice: specific regulation by the ERK1/2, but not JNK, MAP kinase pathway. Psychopharmacology (Berl) 204 135 PMID: 19125235
Chen-Roetling et al (2009) Heme oxygenase activity and hemoglobin neurotoxicity are attenuated by inhibitors of the MEK/ERK pathway. Neuropharmacology 56 922 PMID: 19371583
Freeman et al (2011) A metabolic perturbation by U0126 identifies a role for glutamine in resveratrol-induced cell death. Cancer Biol Ther 12 966 PMID: 22108021
Urs et al (2011) A DA D1 receptor-dependent β-arrestin signaling complex potentially regulates morphine-induced psychomotor activation but not reward in mice. Neuropsychopharmacology 36 551 PMID: 20980993
Subramanian and Morozov (2011) Erk1/2 inhibit synaptic vesicle exocytosis through L-type calcium channels. J Neurosci 31 4755 PMID: 21430174
Oh et al (2017) Negative regulation of ERK1/2 by PI3K is required for the protective effects of Pyropia yezoensis peptide against perfluorooctane sulfonate-induced endoplasmic reticulum stress. Mol Med Rep 15 2583 PMID: 28260037
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481
Lee et al (2014) Mechanism and treatment for learning and memory deficits in mouse models of Noonan syndrome. Nat Neurosci 17 1736 PMID: 25383899
Seese et al (2014) Spaced training rescues memory and ERK1/2 signaling in fragile X syndrome model mice. Proc Natl Acad Sci U S A 111 16907 PMID: 25385607
Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469
Osterweil et al (2010) Hypersensitivity to mGluR5 and ERK1/2 leads to excessive protein synthesis in the hippocampus of a mouse model of fragile X syndrome. J Neurosci 30 15616 PMID: 21084617
Beaulieu et al (2005) An Akt/beta-arrestin 2/PP2A signaling complex mediates DArgic neurotransmission and behavior. Cell 122 261 PMID: 16051150
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Literature in this Area
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MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.