Product Introduction
Bioactivity


英文名: 1-Azakenpaullone

描述: 1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂，其 IC50=18 nM。

细胞实验: Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. The relative cell number is determined after treatment with 1-Azakenpaullone for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control. (Only for Reference)

激酶实验: Kinase preparations and assays: GSK-3β is assayed, following a 1/100 dilution in 1 mg BSA per mL 10 mM dithiothreitol, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol-1; 1 mCi·mL-1 ) in a final volume of 30 μL. After 30 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto 2.5×3 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed five times in a solution of 10 mL phosphoric acid per L of water. The wet filters are counted in the presence of 1 mL ACS scintillation fluid. The kinase activity of CDK1/cyclin B is assayed in buffer C, with 1 mg/mL histone H1, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol-1; 1 mCi·mL-1 ) in a final volume of 30 μL. After 10 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. The activity of CDK5/p25 is assayed in buffer C as described for CDK1/cyclin B. (Buffer A: 10 mM MgCl2 , 1 mM EGTA, 1 mM dithiothreitol, 25 mM Tris/HCl pH 7.5, 50 μg heparin/mL. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)

体外活性: 1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. [1] In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. [2] 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. [3][4]

体内活性: Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive de?cits, and improves the ketamine-induced motor incoordination in rotarod test. [5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 61 mg/mL (185.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Glycogen synthase kinase-3 | 1 Azakenpaullone | GSK-3 | 1Azakenpaullone | Glycogen synthase kinase 3 | Inhibitor | 1-Azakenpaullone | inhibit | 1-Akp

相关产品: Cromolyn sodium | ABC1183 | CDK8-IN-12 | PHA-767491 | GSK-3 inhibitor 1 | GSK-3β inhibitor 1 | MeBIO | GS87 | SB 415286 | CCG 203769

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