SL 327

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Cat.No. 1969 - SL 327 | C16H12F3N3S | CAS No. 305350-87-2
Description: Selective inhibitor of MEK1 and MEK2; brain penetrant
Chemical Name: α-[Amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitrile
Purity: ≥99% (HPLC)
Datasheet
Citations (9)
Literature
Pathways

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.

Compound Libraries

SL 327 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 335.35
Formula C16H12F3N3S
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 305350-87-2
PubChem ID 9549284
InChI Key JLOXTZFYJNCPIS-FYWRMAATSA-N
Smiles N\C(SC1=CC=C(N)C=C1)=C(\C#N)C1=CC=CC=C1C(F)(F)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.53 100
ethanol 16.77 50

Preparing Stock Solutions

The following data is based on the product molecular weight 335.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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:


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Keywords: Selective inhibitors inhibits MEK1 MEK2 brain penetrant Mitogen-Activated Protein Kinase MEK Kinases SL327 MEK

9 Citations for SL 327

Citations are publications that use Tocris products. Selected citations for SL 327 include:

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

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

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

Urs et al (2011) A dopamine D1 receptor-dependent β-arrestin signaling complex potentially regulates morphine-induced psychomotor activation but not reward in mice. Neuropsychopharmacology 36 551 PMID: 20980993

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

Subramanian and Morozov (2011) Erk1/2 inhibit synaptic vesicle exocytosis through L-type calcium channels. J Neurosci 31 4755 PMID: 21430174

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


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Pathways for SL 327

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

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