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

LY2090314 

Cat. No.: HY-16294 Purity: 99.73%
Data Sheet SDS Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $135 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg $550 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

    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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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.

    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 Vemurafenib and has an independent mechanism of action[2].

    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].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01287520 Eli Lilly and Company Advanced Cancer November 2007 Phase 1
    NCT01632306 Eli Lilly and Company|Mayo Clinic Pancreatic Cancer March 2013 Phase 1|Phase 2
    NCT01214603 Eli Lilly and Company Leukemia November 2010 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    10 mM 0.1951 mL 0.9756 mL 1.9511 mL
    Animal Administration
    [2]

    LY2090314 is formulated in 20% Captisol/0.01N HCl.

    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
    Molecular Weight

    512.53

    Formula

    C₂₈H₂₅FN₆O₃

    CAS No.

    603288-22-8

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.73%

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    Product Name:
    LY2090314
    Cat. No.:
    HY-16294
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