LY2090314

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Technical Data

Molecular Weight 512.53 Storage powder
Formula

C28H25FN6O3

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CAS No. 603288-22-8 Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (195.11 mM)
Ethanol 2 mg/mL warmed (3.9 mM)
Water Insoluble
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.
Chemical Name 3-(9-fluoro-2-(piperidine-1-carbonyl)-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

Biological Activity

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.
Targets
GSK-3β [1] GSK-3α [1]
0.9 nM 1.5 nM
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. [1]
In vivo LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts. [1]
Features  
 

References

Customer Product Validation

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.

LY2090314 has been referenced in 1 publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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