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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 497 | 现货 | |
2 mg | ¥ 747 | 现货 | |
5 mg | ¥ 1,660 | 现货 | |
10 mg | ¥ 2,660 | 现货 | |
25 mg | ¥ 4,890 | 现货 | |
50 mg | ¥ 6,930 | 现货 | |
100 mg | ¥ 9,530 | 现货 | |
500 mg | ¥ 18,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,780 | 现货 |
产品描述 | 1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. |
靶点活性 | GSK-3β:18 nM |
体外活性 | 1-Azakenpaullone有效地抑制CDK1/cyclin B、CDK5/p25和GSK-3β,其IC50分别为0.018 μM、4.2 μM和2.0 μM。[1] 在人类胰岛中,1-Azakenpaullone (5 mM)与葡萄糖(8 mM)结合,刺激β细胞增殖。[2] 1-Azakenpaullone有效促进INS-1E细胞复制,并保护INS-1E细胞免受糖脂毒性诱导的细胞死亡。[3][4] |
体内活性 | 1-Azakenpaullone(10或100 pmol, i.c.v.)能够减轻氯胺酮引起的运动过度活跃、PPI中断和认知缺陷,并改善氯胺酮在转棒试验中引起的运动协调障碍。[5] |
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.) |
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) |
别名 | azakenpaullone, 1-氮杂坎帕罗酮 |
分子量 | 328.16 |
分子式 | C15H10BrN3O |
CAS No. | 676596-65-9 |
Smiles | Brc1ccc2[nH]c-3c(CC(=O)Nc4cccnc-34)c2c1 |
密度 | 1.655 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (182.84 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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