1-氮杂坎帕罗酮
货号：
IA2800
品牌：
Jinpan
暂无详情
产品简介
| MDL | MFCD09037522 |
| 描述 | 是具有高度选择性的、ATP 竞争性的糖原合成酶激酶3 β (GSK-3β) 的抑制剂。 |
| EC | EINECS 200-258-5 |
| 别名 | 1-Azakenpaullone |
| 英文名称 | 1-Azakenpaullone |
| CAS | 676596-65-9 |
| 分子式 | C15 H10 Br N3 O |
| 分子量 | 328.16 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | 1-Azakenpaullone可选择性抑制CDK1/cyclin B、CDK5/p25和GSK-3β活性, IC50值分别为0.018 μM、 4.2 μM和2.0 μM。[1] |
| In Vitro | 在人胰岛细胞中，1-Azakenpaullone (5 mM)和葡萄糖 (8 mM)联合可抑制β细胞的增殖。[2] 1-Azakenpaullone可有效诱导INS-1E细胞复制，并保护INS-1E细胞免于脂糖毒性引起的细胞死亡。[3][4] |
| In Vivo | 1-Azakenpaullone (10 或100 pmol, 脑内注射)预处理可减弱克他命引起的运动亢进、PPI中断、认知缺陷，并在转动试验中提高克他命引起的运动不协调。 |
| 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.)[6] |
| SMILES | O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4 |
| 靶点 | GSK-3 |
| 动物实验 | Cell lines: INS-1E β细胞系;Concentrations: 20 μM;Incubation Time: 4 天[4] |
| 细胞实验 | Animal Models: 雄性 NMRI小鼠;Dosages: ~500 pmol;Administration: 脑内注射[5] |
| 数据来源文献 | [1] Kunick C, et al. Bioorg Med Chem Lett. 2004, 14(2), 413-416. [2] Liu H, et al. Diabetes. 2009, 58(3), 663-672. [3] Stukenbrock H, et al. J Med Chem. 2008, 51(7), 2196-2207. [4] Mussmann R, et al. J Biol Chem. 2007, 282(16), 12030-12037. [5] Chan MH, et al. Schizophr Res. 2012, 136(1-3), 96-103. [6] Leost M, et al. Eur J Biochem. 2000, 267(19), 5983-5994. |
| 规格 | 2mg |
是一种高度选择性GSK-3β抑制剂。