2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. LY2090314

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

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

LY2090314 Chemical Structure

LY2090314 Chemical Structure

CAS No. : 603288-22-8

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 135 In-stock
Solution
10 mM * 1 mL in DMSO USD 135 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
50 mg USD 550 In-stock
100 mg USD 880 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

LY2090314 Related Antibodies

Top Publications Citing Use of Products

    LY2090314 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2018 Dec 11;11(6):1539-1550.  [Abstract]

    The CDX2 protein expression levels are measured by western blotting analysis in the treatment of SB216763, CHIR99021, LY2090314, BIO and BIO.DAPT.

    LY2090314 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2018 Dec 11;11(6):1539-1550.  [Abstract]

    Immunostaining analysis of CDX2 (green) is performed in the human iPSC-derived intestinal progenitor cells in the treatment of LY2090314.

    LY2090314 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2016 Dec 23;291(52):26875-26885.  [Abstract]

    K562 cells expressing wild-type S-UNG2 are treated with the GSK-3 inhibitor LY2090314 (LY) for 90 min. Phosphorylation of UNG2 is detected with phospho-PLK1 motif antibody (top). UNG2 expression in input cell lysates is detected by Western blotting for the S tag (bottom).

    View All GSK-3 Isoform Specific Products:

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    GSK-3 GSK-3α GSK-3β

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

    IC50 & Target[1]

    GSK-3β

    0.9 nM (IC50)

    GSK-3α

    1.5 nM (IC50)

    In Vitro

    LY2090314 (20 nM) promotes a time-dependent stabilization of β-catenin total protein as well as an induction of Axin2. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases. LY2090314 potently induces apoptotic cell death in a panel of melanoma cell lines irrespective of BRAF mutation status. Cell death induced by LY2090314 is dependent on β-catenin and GSK3β knockdown increases the sensitivity of cells to LY2090314. LY2090314 remains active in cell lines resistant to PLX4032 and has an independent mechanism of action[2].

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

    LY2090314 Related Antibodies
    In Vivo

    LY2090314 exhibits high clearance (approximating hepatic blood flow) and a moderate volume of distribution (appr 1-2 L/kg) resulting in rapid elimination (half-life appr 0.4, 0.7, and 1.8-3.4 hours in rats, dogs, and humans, respectively). LY2090314 is rapidly cleared by extensive metabolism with negligible circulating metabolite exposures due to biliary excretion of metabolites into feces with no apparent intestinal reabsorption[1].
    LY2090314 (25 mg/kg Q3D, i.v.) elevates Axin2 gene expression in vivo, demonstrates single agent activity in the A375 xenograft model of melanoma and enhances the efficacy of DTIC[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    512.53

    Formula

    C28H25FN6O3
    CAS No.
    Appearance

    Solid

    Color

    Orange to reddish brown

    SMILES

    O=C(C(C1=CN2CCN(C(N3CCCCC3)=O)CC4=CC(F)=CC1=C42)=C5C6=CN=C7C=CC=CN76)NC5=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9511 mL 9.7555 mL 19.5111 mL
    5 mM 0.3902 mL 1.9511 mL 3.9022 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 1.25 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 1.25 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  20% HP-β-CD/10 mM Citrate pH 2.0

      Solubility: 10 mg/mL (19.51 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.85%

    SDS (392 KB)

    COA (264 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [2]

    Five million A375 human melanoma cancer cells are injected S.C. in the flank of female 6 to 8 week old athymic nude mice in a 1:1 mixture with matrigel. Mice are monitored daily for palpable tumors. When tumors reach appr 100 mm2 mice are randomized into groups receiving either LY2090314 (25 mg/kg Q3D) or vehicle (20% Captisol/0.01N HCl) via i.v. administration. Tumor volume (measured by calipers) and animal body weight are recorded twice weekly. Tumor volumes are calculated using the formula: (a2 × b)/2 (a being the smaller and b being the larger dimension of the tumor). For combination studies with DTIC (60 mg/kg QD), LY2090314 is dosed at 2.5 mg/kg Q3D and tumor growth monitored.

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9511 mL 9.7555 mL 19.5111 mL 48.7776 mL
    5 mM 0.3902 mL 1.9511 mL 3.9022 mL 9.7555 mL
    10 mM 0.1951 mL 0.9756 mL 1.9511 mL 4.8778 mL
    15 mM 0.1301 mL 0.6504 mL 1.3007 mL 3.2518 mL
    20 mM 0.0976 mL 0.4878 mL 0.9756 mL 2.4389 mL
    25 mM 0.0780 mL 0.3902 mL 0.7804 mL 1.9511 mL
    30 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6259 mL
    40 mM 0.0488 mL 0.2439 mL 0.4878 mL 1.2194 mL
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    LY2090314 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LY2090314603288-22-8LY 2090314LY-2090314GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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