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    InvivoChem Cat #: V0456
    CAS #: 305350-87-2Purity ≥98%

    Description: SL327 (SL-327) is a novel, potent and selective inhibitor for MEK1/2 with the ability to cross blood brain barrier and block fear conditioning. It inhibits MEK1/2 with IC50s of 0.18 μM/ 0.22μM, and shows little/no activity towards Erk1, MKK3, MKK4, c-JUN, PKC, PKA, or CamKII. SL327 blocks acquisition but not expression of lithium-induced conditioned place aversion: a behavioral and immunohistochemical study. SL327 had no affect on acquisition, expression, or extinction of EtOH-induced CPP in mice despite causing significant reduction of pERK levels in multiple brain regions.

    References: J Biol Chem. 2000 Nov 24;275(47):37086-92; J Neurosci. 2000 Dec 1;20(23):8701-9.

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    Molecular Weight (MW)335.35
    CAS No.305350-87-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 67 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: 7 mg/mL (20.9 mM)
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL

    SL 327; SL-327; SL327

    Chemical Name: (E)-3-amino-3-((4-aminophenyl)thio)-2-(2-(trifluoromethyl)phenyl)acrylonitrile


    InChi Code: InChI=1S/C16H12F3N3S/c17-16(18,19)14-4-2-1-3-12(14)13(9-20)15(22)23-11-7-5-10(21)6-8-11/h1-8H,21-22H2/b15-13-

    SMILES Code: N#C/C(C1=CC=CC=C1C(F)(F)F)=C(N)/SC2=CC=C(N)C=C2 

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    In Vitro

    In vitro activity: SL327 is a water soluble, structural homologue of the specific MKK1/2 inhibitor U0126 with IC50 of 0.18 μM and 0.22 μM for MEK1 and MEK2 respectively. SL327 has no effect on a variety of other kinases, including PKA, PKC, or CamKII.

    Kinase Assay: Protein kinase assays are performed. All kinase assays are started by adding enzyme to a mixture that included [γ-32P]ATP and substrate. This mixture is then incubated at 30°C or 37°C for 10 min. The reaction is stopped by spotting aliquots of the reaction mixture onto Whatman P-81 phosphocellulose filter paper. The papers are then washed in 150 mM H3PO4, dried, and subjected to scintillation counting. The catalytic subunit of PKA is assayed by measuring [32P]phosphate incorporation into the substrate Kemptide (100 μM). The activity of CaMKII is determined by measuring phosphorylation of the synthetic peptide Autocamtide (100 μM) in the presence of 100 μM Calcium and 10 μg/mL Calmodulin. A synthetic peptide analog of a fragment of neurogranin, NG(28-43) (10 μM) is used as a specific substrate for the catalytic subunit of PKC. In all cases, substrate phosphorylation was linear with respect to time and enzyme concentration. 

    In VivoSL327 (50 mg/kg) crosses the blood-brain barrierand and blocks fear conditioning by inhibiting MAPK/ERK phosphorylation. SL327 (30 mg/kg) significantly impairs spatial learning in mice. SL327 (50 mg/kg) blocks cocaine-induced properties
    Animal modelFear conditioning experiments in male Spague-Dawley rats.
    Formulation & DosageDissolved in DMSO; 10-100 mg/Kg; i.p. injection
    ReferencesJ Biol Chem. 2000 Nov 24;275(47):37086-92; J Neurosci. 2000 Dec 1;20(23):8701-9.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


     2016 Jun;124:40-7.


     2016 Jun;124:40-7.


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