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LY2090314

Chemical Structure : LY2090314

CAS No.: 603288-22-8

LY2090314 (LY 2090314)

Catalog No.: PC-20193Not For Human Use, Lab Use Only.

LY2090314 is a potent and selective ATP-competitive inhibitor of Glycogen synthase kinase-3 (GSK-3) with IC50 of 1.5/0.9 nM for GSK3α/GSK3β, respectively.

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25 mg $328 In stock
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100 mg $928 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY2090314 is a potent and selective ATP-competitive inhibitor of Glycogen synthase kinase-3 (GSK-3) with IC50 of 1.5/0.9 nM for GSK3α/GSK3β, respectively.
LY2090314 stimulated TCF/LEF TOPFlash reporter activity, stabilized β-catenin and elevated the expression of Axin2 in a panel of melanoma cell lines at nM potency.
LY2090314 exhibited cytotoxicity against melanoma cell lines in vitro with IC50 of 10 nM, but not other solid tumor cell lines (IC50 >10 uM).
LY2090314 elevates Axin2 gene expression after a single dose and produces tumor growth delay in A375 melanoma xenografts with repeat dosing.

Physicochemical Properties

M.Wt 512.55
Formula C28H25FN6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[9-fluoro-2-(piperidin-1-ylcarbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-4-imidazo[1,2-a]pyridin-3-yl-1H-pyrrole-2,5-dione

References

1. Atkinson JM, et al. PLoS One. 2015 Apr 27;10(4):e0125028.

2. Rizzieri DA, et al. Leuk Lymphoma. 2016 Aug;57(8):1800-6.

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