SL 327

Catalog # Availability Size / Price Qty
1969/10
1969/1
1969/50
SL 327 | CAS No. 305350-87-2 | MEK Inhibitors
1 Image
Description: Selective inhibitor of MEK1 and MEK2; brain penetrant

Chemical Name: α-[Amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitrile

Purity: ≥99%

Product Details
Citations (20)
Reviews

Biological Activity

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

M.Wt:
335.35
Formula:
C16H12F3N3S
Solubility:
Soluble to 50 mM in ethanol and to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
305350-87-2

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.

Background References

  1. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  2. 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.
    J.Neurosci., 2000;20:4563
  3. Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy.
    Scherle et al.
    J.Biol.Chem., 2000;275:37086
  4. 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.
    J.Pharmacol.Exp.Ther., 2003;304:172
  5. The MAPK cascade is required for mammalian associative learning.
    Atkins et al.
    Nature Neurosci., 1998;1:602

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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

  1. 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
  2. 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
  3. Cell type-dependent Erk-Akt pathway crosstalk regulates the proliferation of fetal neural progenitor cells
    Authors: Rhim Et al.
    Scientific Reports  2016;6:26547
  4. Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
    Authors: Liddell Et al.
    J Neuroinflammation  2016;13:49
  5. 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
  6. 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
  7. G Protein and β-arrestin signaling bias at the ghrelin receptor.
    Authors: Evron Et al.
    J Biol Chem  2014;289:33442
  8. Mechanism and treatment for learning and memory deficits in mouse models of Noonan syndrome.
    Authors: Lee Et al.
    Nat Neurosci  2014;17:1736
  9. 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
  10. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal  2013;11:35
  11. A DA D1 receptor-dependent β-arrestin signaling complex potentially regulates morphine-induced psychomotor activation but not reward in mice.
    Authors: Urs Et al.
    Neuropsychopharmacology  2011;36:551
  12. Erk1/2 inhibit synaptic vesicle exocytosis through L-type calcium channels.
    Authors: Subramanian and Morozov
    J Neurosci  2011;31:4755
  13. 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
  14. 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
  15. Genetic targeting of ERK1 suggests a predominant role for ERK2 in murine pain models.
    Authors: Alter Et al.
    J Neurosci  2010;30:11537
  16. Heme oxygenase activity and hemoglobin neurotoxicity are attenuated by inhibitors of the MEK/ERK pathway.
    Authors: Chen-Roetling Et al.
    Neuropharmacology  2009;56:922
  17. 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
  18. 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
  19. Paradoxical striatal cellular signaling responses to psychostimulants in hyperactive mice.
    Authors: Beaulieu Et al.
    Neuropsychopharmacology  2006;281:32072
  20. An Akt/beta-arrestin 2/PP2A signaling complex mediates DArgic neurotransmission and behavior.
    Authors: Beaulieu Et al.
    Cell  2005;122:261

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