LY2090314 (GMP) is LY2090314 (HY-16294) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
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- CAS No.: 603288-22-8
- Formule: C28H25FN6O3
- Masse moléculaire:512.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
LY2090314 (GMP) (20 nM) promotes a time-dependent stabilization of β-catenin total protein as well as an induction of Axin2. LY2090314 (GMP) is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases. LY2090314 (GMP) potently induces apoptotic cell death in a panel of melanoma cell lines irrespective of BRAF mutation status. Cell death induced by (GMP) is dependent on β-catenin and GSK3β knockdown increases the sensitivity of cells to (GMP). (GMP) 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. .
In Vivo
LY2090314 (GMP) (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.
Chemical Information
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CAS No. 603288-22-8
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Masse moléculaire 512.53
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Formule C28H25FN6O3
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SMILES
O=C(C(C1=CN2CCN(C(N3CCCCC3)=O)CC4=CC(F)=CC1=C42)=C5C6=CN=C7C=CC=CN76)NC5=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Atkinson JM, et al. Activating the Wnt/β-Catenin Pathway for the Treatment of Melanoma--Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3. PLoS One. 2015 Apr 27;10(4):e0125028. [Content Brief]
[2]. Zamek-Gliszczynski MJ, et al. Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. Dr [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY2090314 (GMP) Related Classifications
HY-16294G Related Classifications
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