化学信息：
| 化学名 | 9-bromo-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one |
|
| 简称 | Kenpaullone | |
| 别名 |
1-azakenpaullone, NSC 664704, NSC-664704, NSC664704 |
|
| 中文名 | N/A | |
| 化学式 | C16H11BrN2O | |
| 分子量 | 327.18 | |
| CAS号 | 142273-20-9 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO65mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.53ml DMSO，或者每3.27mg加入1ml DMSO，配制成10mM溶液。SC6610-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Kenpaullone is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23µM. | ||||
| 信号通路 | Cell Cycle | ||||
| 靶点 | GSK-3β | CDK1/CyclinB | CDK2/CyclinA | CDK5/p35 | CDK2/CyclinE |
| IC50 | 0.23μM | 0.4μM | 0.68μM | 0.85μM | 7.5μM |
| 体外研究 | In HEK-293 cells, phosphorylation of the endogenous GSK3α on Tyr279 is greatly decreased after prolonged incubation with Kenpaullone. Also, the Phosphorylation of the endogenous GSK3β also decreases, although less markedly. Kenpaullone also induces the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. Kenpaullone (20µM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli. | ||||
| 体内研究 | N/A | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | HEK-293 cells |
| 浓度 | 10μM |
| 处理时间 | 0-12h |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SC6610-10mM | Kenpaullone (CDK抑制剂) | 10mM×0.2ml |
| SC6610-5mg | Kenpaullone (CDK抑制剂) | 5mg |
| SC6610-25mg | Kenpaullone (CDK抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
