1. PI3K/Akt/mTOR
    Stem Cell/Wnt
    Apoptosis
  2. GSK-3
    Apoptosis
  3. SB 415286

SB 415286 

Cat. No.: HY-15438 Purity: 99.72%
Handling Instructions

SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.

For research use only. We do not sell to patients.

SB 415286 Chemical Structure

SB 415286 Chemical Structure

CAS No. : 264218-23-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 320 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SB 415286 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 7;8(47):82174-82184.

    Comparisons of β-catenin and QKI-5 levels between H1299-vector and H1299-QKI-5 cells in which β-catenin degradation is blocked with proteasome inhibitor MG132 or GSK3β inhibitor SB415286 (25 μM).

    View All GSK-3 Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.

    IC50 & Target[1]

    hGSK-3α

    77.5 nM (IC50)

    hGSK-3β

    77.5 nM (IC50)

    In Vitro

    SB 415286 (SB-415286) inhibits human GSK-3α with an IC50 of 77.5 nM, and a Ki of 30.75 nM. SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with EC50 of 2.9 μM. SB-415286 stimulates glycogen synthase activity in Chang human liver cells. SB-415286 induces transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells[1]. SB 415286 (SB-415286, 5-44 μM) attenuates B65 cell loss mediated by 1 mM H2O2. SB-415286 (5-44 μM) causes a significant dose-dependent decrease in the fluorescence intensity of DCF, and attenuates B65 ROS production as mediated by 1 mM H2O2. SB-415286 (5-44 μM) also attenuates ROS production in CGN mediated by 1 mM H2O2[2]. SB-415286 (50 µM) induces a substantial suppression of immunoprecipitated GSK3 activity by 97%[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    359.72

    Formula

    C₁₆H₁₀ClN₃O₅

    CAS No.

    264218-23-7

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (277.99 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7799 mL 13.8997 mL 27.7994 mL
    5 mM 0.5560 mL 2.7799 mL 5.5599 mL
    10 mM 0.2780 mL 1.3900 mL 2.7799 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    GSK-3 kinase activity is measured, in the presence or absence of SB-216763 or SB-415286, in a reaction mixture containing final concentrations of: 1 nM human GSK-3α or rabbit GSK3α; 50 mM MOPS pH 7.0; 0.2 mM EDTA; 10 mM Mg-acetate; 7.5 mM β-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 ranges from 0 to 45 μM (Ki determinations). Following 30 min 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    B65 cells are used after 24 h of in vitro culture. CGN are used after 7-8 days in vitro. Lithium and SB-415286 are dissolved in culture media and DMSO, respectively, and added to the neuronal preparation at the precise concentrations, 1 h before addition H2O2 (50 μM to 1 mM). To assess the loss in cell viability, we use the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium] method. MTT is added to the cells at a final concentration of 250 μM and incubated for 1 h, allowing the reduction in MTT to produce a dark blue formazan product. Media are then removed, and cells are dissolved in dimethylsulfoxide. Formazan production is measured by the absorbency change at 595 nm using a microplate reader. Viability results are expressed as percentages. The absorbency measured from non-treated cells is taken to be 100%[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.72%

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    Keywords:

    SB 415286SB415286SB-415286GSK-3ApoptosisGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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    Product Name:
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