product name 1-Azakenpaullone
Description: 1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, it displayed >100-fold selectivity over CDK1/cyclin B and CDK5/p25. As an inhibitor of GSK-3β, 1-Azakenpaullone is developed as potential antidiabetic drug. 1-Azakenpaullone is found to protect rat insulinoma cell line INS-1E cells from glucolipotoxicity and stimulate cell proliferation. Besides that, 1-Azakenpaullone promotes the replication of beta cells in isolated rat islets at concentration of 1μM.
References: J Med Chem. 2008 Apr 10;51(7):2196-207; Eur J Biochem. 2000 Oct;267(19):5983-94; J Biol Chem. 2007 Apr 20;282(16):12030-7.
512.53
Formula
C28H25FN6O3
CAS No.
603288-22-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (195.1 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL warmed (3.9 mM)
Solubility (In vivo)
Synonyms
LY 2090314; LY-2090314
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424025
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: The IC50 values for CDK1/cyclin B, CDK5/p25 and GSK-3β are 2μM, 4.2μM and 18nM, respectively. As an inhibitor of GSK-3β, 1-Azakenpaullone is developed as potential antidiabetic drug. 1-Azakenpaullone is found to protect rat insulinoma cell line INS-1E cells from glucolipotoxicity and stimulate cell proliferation. Besides that, 1-Azakenpaullone promotes the replication of beta cells in isolated rat islets at concentration of 1μM. In addition, 1-Azakenpaullone is reported to have effect in changing cardiac myocyte morphology. It increases cell area primarily through the elongation of the cells. |
|---|---|
| In Vivo | LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2008 Apr 10;51(7):2196-207; Eur J Biochem. 2000 Oct;267(19):5983-94; J Biol Chem. 2007 Apr 20;282(16):12030-7. |
