| 产品描述: | Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line |
| 靶点: |
Cdk1/cyclin B:35 nM (IC50);cdk2/cyclin A:15 nM (IC50);CDK2/Cyc E:200 nM (IC50);CDK5/p35:40 nM (IC50);GSK-3α:4 (IC50);GSK-3β:4 nM (IC50) |
| 体内研究: |
Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts. Animal Model: 5-6 week old athymic nude mice Dosage: 30 mg/kg Administration: Subcutaneous injections, daily for 2 weeks Result: Antitumor effect in Group 3 medulloblastomas. |
| 参考文献: |
1. Leost M, et al. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267(19):5983-94. 2. Lahusen T, et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36(4):183-94. 3. Chunying Cui, et al. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect. J Anal Methods Chem. 2013;2013:602091. 4. Claudia C Faria, et al. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma. Oncotarget. 2015 Aug 28;6(25):21718-29. |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.41 ml |
17.049 ml |
34.097 ml |
| 5 mM |
0.682 ml |
3.41 ml |
6.819 ml |
| 10 mM |
0.341 ml |
1.705 ml |
3.41 ml |
| 50 mM |
0.068 ml |
0.341 ml |
0.682 ml |
|
| 注意: |
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