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    SB415286
    SB415286

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0216
    CAS #: 264218-23-7Purity ≥98%

    Description: SB415286 is a novel, potent, selective, cell permeable and ATP-competitive GSK3α (glycogen synthase kinase-3alpha) inhibitor with potential anti-inflammatory activity. It inhibits GSK3α with an IC50/Ki of 78 nM/31 nM and has equal inhibitory against GSK-3β. SB-415286 inhibited GSK-3 activity and promoted glycogen synthesis in human liver cells and induced expression of reporter gene regulated by catenin-LEF/TCF in HEK293 cells. In primary neurons, it can prevent cell death induced by repressed PI3k pathway activity. Further studies showed that reduced GSK3β activity induced by SB-415286 could inhibit down-regulation of cyclin D1, cell cycle arrest and chemosensitivity, which were all mediated by rapamycin. Glycogen synthase kinase-3β (GSK-3β) is a multifunctional serine/threonine kinase that plays important roles in the necrosis and apoptosis of cardiomyocytes.

    References: Chem Biol. 2000 Oct;7(10):793-803; J Neurooncol. 2011 Aug;104(1):145-53.

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    Molecular Weight (MW)

    359.72

    Formula

    C16H10ClN3O5

    CAS No.

    264218-23-7

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 72 mg/mL (200.2 mM)       

    Water: <1 mg/mL

    Ethanol: 72 mg/mL (200.2 mM)      

    SMILES

     O=C(C(NC1=CC=C(O)C(Cl)=C1)=C2C3=CC=CC=C3[N+]([O-])=O)NC2=O

    Synonyms

    SB-415286; SB415286; SB 415286.

    Chemical Name: 3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione

    SMILES Code: O=C(C(NC1=CC=C(O)C(Cl)=C1)=C2C3=CC=CC=C3[N+]([O-])=O)NC2=O



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    In Vitro

    In vitro activity: SB 415286 inhibits GSK3α in an ATP competitive manner with Ki of 31 nM and shows similar potency against GSK3β. SB 415286 has little or no activity against 24 other protein kinases with IC50 > 10 μ M. SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with EC50 of 2.9 μM, and induces expression of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells. SB 415286 protects both central and peripheral nervous system neurones in culture from death induced by reduced PI3-kinase pathway activity in a concentration-dependent manner, which is correlated with inhibition of GSK-3 activity and modulation of GSK-3 substrates tau and β-catenin. In L6 myotubes, SB 415286 induces a much greater activation of GS (6.8-fold) compared to that elicited by insulin (4.2-fold) or Li (4-fold). SB 415286 (10 μM) inhibits rapamycin-induced down-regulation of cyclin D1, and blocks rapamycin and paclitaxel-induced apoptosis, suggesting a critical role for GSK3β in rapamycin-mediated paclitaxel-sensitization. SB 415286 prevents coxsackievirus-induced cell death in a dose-dependent manner via stabilization of β-catenin

     

    Kinase Assay: GSK-3 kinase activity is measured, in the presence of various concentrations of SB 415286, in a reaction mixture containing final concentrations of: 1 nM human GSK3α or rabbit GSK3α; 50 mM MOPS pH 7.0; 0.2 mM EDTA; 10 mM Mg-acetate; 7.5 mM L-mercaptoethanol; 5% (w/v) glycerol; 0.01% (w/v) Tween-20; 10% (v/v) DMSO; 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP (IC50 determinations) or 2.7 μCi [33P]γ-ATP (Ki determinations). The total ATP concentration is 10 μM (IC50 determinations) or ranged from 0 to 45 μM (Ki determinations). Following 30 minutes incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and these are washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter. 

     

    Cell Assay: Cells are exposed to different concentrations of SB 415286 for 48 or 72 hours in 96-flat well plates. After 48 or 72 hours, [3H]thymidine is added to the cultures (10 μCi/well) for the last 12 hours. The [3H]thymidine incorporation is evaluated by scintillation counting by using a top count β-counter. Apoptosis is assessed by annexin V/Propidium Iodide staining or by detection of mitochondrial membrane potential. Cell death is evaluated by the analysis of Forward/Side scatter fluorescence changes. Fluorescence Activated Cell Sorting (FACS) analysis is performed using a FACS-Calibur Cell Cytometer.

    In Vivo

    Administration of SB 415286 (~10 mg/kg twice daily) reduces the extent and degree of the trinitrobenzene sulphonic acid (TNBS)-provoked colonic inflammation in the rat, and reduces the fall in body weight, which is related to downregulation of NF-κB activity, involved in the generation of proinflammatory mediators. SB 415286 treatment at 1 mg/kg significantly delays the growth of Neuro-2A cells in vivo in nude mice.

    Animal model

    Male Wistar rats with acute colitis provoked by trinitrobenzene sulphonic acid (TNBS)

    Formulation & Dosage

    Dissolved in DMSO; 1mg/kg; s.c. injection

    References

    Chem Biol. 2000 Oct;7(10):793-803; J Neurooncol. 2011 Aug;104(1):145-53.



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

    SB415286

    GSK-3β inhibition alters the expression of anti-apoptotic proteins. J Neurooncol. 2011 Aug; 104(1): 145–153.

    SB415286

    GSK-3β inhibition induces G2/M accumulation in Neuro-2A.

    SB415286

    GSK-3β inhibition results in in vivo tumor growth delay.



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