LY2090314

Catalog No.S7063

LY2090314 Chemical Structure

Molecular Weight(MW): 512.53

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.

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1 Customer Review

  • (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.

    Mol Cancer Ther, 2016, 15(7):1485-94.. LY2090314 purchased from Selleck.

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Choose Selective GSK-3 Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SY5Y cells NFfhWpBHfW6ldHnvckBie3OjeR?= M4fCPGlvcGmkaYTpc44hd2ZiR3z5Z49o\W5ic4nueIhie2Via3nuZZNmNTNiYnX0ZUBl\XCnbnTlcpQhXGG3IIDyc5RmcW5ic3XybY5mNTN7NjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iU2m1XUBk\WyuczygTWM2OD1yLkegcm0> NWC0PG9pOTV{NkeyN|I>

... Click to View More Cell Line Experimental Data

In vivo LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts. [1]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (195.11 mM)
Ethanol 2 mg/mL warmed (3.9 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
17mg/mL

* 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 Information

Molecular Weight 512.53
Formula

C28H25FN6O3

CAS No. 603288-22-8
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I want to use BI2536 in preclinical studies using mice with intracranial xenografts. How could I reconstitute the compound?

  • Answer:

    For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BII2536 in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference: http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6 (supplemental Data)

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GSK-3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID