Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
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||
10 mM in DMSO
|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|
AR-A014418 is a selective and effective GSK3(beta) inhibitor with an IC 50 value of 104 (addition)/- 27 nM; no significant inhibition on 26 other kinases.
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor of GSK3(alpha) and GSK3(beta) with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.
AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway.
Bikinin(Abrasin) is a potent inhibitor of plant GSK-3/Shaggy-like kinase; activates BR signaling downstream of the BR receptor.
6-BIO(6-Bromoindirubin-3(acute)-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3(alpha)(beta)/CDK1/CDK5 respectively.
CHIR-98014 is a selective GSK3 inhibitor with IC50s of 0.65 nM and 0.58 nM for GSK-3(alpha) and GSK-3(beta); potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
CHIR-99021 (CT99021) is a GSK-3(alpha)/(beta) inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
GSK-3 inhibitor 1 is a potent GSK-3 inhibitor.
IM-12 is a potent GSK-3(beta) inhibitor with IC50 of 53 nM; shows a significant activity in several biological tests which was comparable or even outplayed the effects of the known SB-216763.
Indirubin-3(acute)-monoxime is a powerful inhibitor of GSK-3(beta) with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM).