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|Solubility (25°C) *||In vitro||DMSO||100 mg/mL (195.11 mM)|
|Ethanol||2 mg/mL warmed (3.9 mM)|
|In vivo||5% DMSO+45% PEG 300+ddH2O||17mg/mL|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.|
|In vitro||LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro. |
|In vivo||LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts. |
Data from [Data independently produced by , , Mol Cancer Ther, 2016, 15(7):1485-94.]
(D) GS87 leads to more effective AML differentiation than other clinically used GSK3 inhibitors. HL-60 cells were treated with GS87 (30 μM), Tideglusib (30 μM) or LY-2090314 (30 μM) for 72 hours and differentiation was measured by the NBT assay. * p<.05; **p<.01.
Data from [Data independently produced by , , Stem Cell Res, 2017, 182-187]
LY2090314 was tested and exhibited similar synergistic apoptotic effect when co-administered with NAC. Error bar represents the standard deviation of 3 biological replicates.
Glycogen synthase kinase-3 inhibition sensitizes human induced pluripotent stem cells to thiol-containing antioxidants induced apoptosis. [Tu C, et al. Stem Cell Res, 2017, 182-187]PubMed: 28772167
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