S87875 |
Alsterpaullone |
MedMol | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)