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LY2090314
Cat No.
CEI-0910
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. Phase 1/2.
CAS No.
603281-60-3
Molecular Weight
494.54
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
GSK-3α, GSK-3β
IC50
1.5 nM; 0.9 nM
Molecular Formula
C28H26N6O3
Chemical Name
1H-Pyrrole-2,5-dione, 3-imidazo[1,2-a]pyridin-3-yl-4-[1,2,3,4-tetrahydro-2-(1-piperidinylcarbonyl)pyrrolo[3,2,1-jk][1,4]benzodiazepin-7-yl]-
Solubility
DMSO mg/mL; Water mg/mL; Ethanol mg/mL
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
LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts.
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