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Products are for research use only. Not for human use. We do not sell to patients.
(LY 2090314; LY-2090314)
LY2090314 Chemical Structure
|Product name: LY2090314|
|Cat. No.: HY-16294|
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50s of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β respectively.
IC50 Value: 1.5 nM (GSK-3α); 0.9 nM (GSK-3β) 
Target: GSK-3α; GSK-3β
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.
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: Even in Mdr1a-, Bcrp-, and Mrp2-knockout rats, LY2090314 metabolites did not appear in circulation, and their urinary excretion was not enhanced, because the hypothesized impaired biliary excretion of metabolites in the absence of these canalicular transporters was not observed. Canine metabolite disposition was generally similar, with the notable exception of dog-unique LY2090314 glucuronide .
Clinical trial: A Study of LY-2090314 and Chemotherapy in Participants With Metastatic Pancreatic Cancer. Phase1/2
|M.Wt||512.53||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 31 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.9511 mL||9.7555 mL||19.5111 mL|
|5 mM||0.3902 mL||1.9511 mL||3.9022 mL|
|10 mM||0.1951 mL||0.9756 mL||1.9511 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|LY2090314||Eli Lilly & Co||Acute myelogenous leukemia||30-NOV-10||31-DEC-12||Phase 2||13-MAY-13|
|Eli Lilly & Co||Metastatic pancreas cancer||31-MAR-13||31-MAY-17||Phase 2||01-OCT-13|
|Eli Lilly & Co||Cancer||30-NOV-07||30-APR-11||Phase 1||02-AUG-11|
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Kenpaullone is an ATP-competitive inhibitor of several CDKs as well as GSK-3(beta), with an IC50 value of 0.23 (mu)M for GSK-3(beta) and 0.4, 0.68, 0.85, and 0.47 (mu)M for CDK1/cyclin B, CDK2/cyclin A, CDK5/p25, and lymphocyte kinase., respectively.
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