LY2090314

Catalog No.S7063 Batch:S706303

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Technical Data

Formula

C28H25FN6O3
Molecular Weight 512.53 CAS No. 603288-22-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (195.11 mM)
Ethanol 2 mg/mL (3.9 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    A375 cells

  • Concentrations

    20 nM

  • Incubation Time

    5 h

  • Method

    Cells were treated with various concentrations of drug for 5 h.
Animal Study:

[2]
  • Animal Models

    Female athymic nude mice

  • Dosages

    25 mg/kg

  • Administration

    i.v

Customer Product Validation

Data from [Data independently produced by , , Cancer Res, 2017, 77(21):5873-5885]

Data from [Data independently produced by , , Mol Cancer Ther, 2016, 15(7):1485-94.]

Data from [Data independently produced by , , Stem Cell Res, 2017, 182-187]

Data from [Data independently produced by , , BMC Cancer, 2018, 18(1):560]

Selleck's LY2090314 has been cited by 28 publications

Integrin-mediated electric axon guidance underlying optic nerve formation in the embryonic chick retina [ Commun Biol, 2023, 6(1):680] PubMed: 37391492
Integrin-mediated electric axon guidance underlying optic nerve formation in the embryonic chick retina [ Commun Biol, 2023, 6(1):680] PubMed: 37391492
Cranial Suture Regeneration Mitigates Skull and Neurocognitive Defects in Craniosynostosis [ Cell, 2021, 184(1):243-256.e18] PubMed: 33417861
ARIH1 signaling promotes anti-tumor immunity by targeting PD-L1 for proteasomal degradation [ Nat Commun, 2021, 12(1):2346] PubMed: 33879767
KARATE: PKA-induced KRAS4B-RHOA-mTORC2 supercomplex phosphorylates AKT in insulin signaling and glucose homeostasis [ Mol Cell, 2021, S1097-2765(21)00735-8] PubMed: 34551282
GSK-3β manipulates ferroptosis sensitivity by dominating iron homeostasis [ Cell Death Discov, 2021, 7(1):334] PubMed: 34732689
A GSK3-SRF Axis Mediates Angiotensin II Induced Endothelin Transcription in Vascular Endothelial Cells [ Front Cell Dev Biol, 2021, 9:698254] PubMed: 34381779
Glycogen synthase kinase-3 beta (GSK3β)-mediated phosphorylation of ETS1 promotes progression of ovarian carcinoma [ Aging (Albany NY), 2021, 13(10):13739-13763] PubMed: 34023818
C81-evoked inhibition of the TNFR1-NFκB pathway during inflammatory processes for stabilization of the impaired vascular endothelial barrier for leukocytes [ FASEB J, 2021, 35(6):e21656] PubMed: 34042211
CMTM8 as an LPA1-associated partner mediates lysophosphatidic acid-induced pancreatic cancer metastasis [ Ann Transl Med, 2021, 9(1):42] PubMed: 33553335

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.