| 货号 | 14428-1mg |
| 描述 | Alsterpaullone is a derivative of kenpaullone (Item No. 10010239), an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK3β). With slightly improved potency over kenpaullone, alsterpaullone selectively inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and GSK3α/β with IC50 values of 35, 15, 200, 40, and 4 nM, respectively.1,2 Alsterpaullone has been used to inhibit the cytosolic degradation of β-catenin to alter the canonical Wnt signaling pathway in primary axis patterning, to reduce tau phosphorylation in an effort to modify neuropathological events associated with Alzheimer’s disease, and to alter cell proliferation or protein expression in various diseases.3,4,5 |
| 别名 | 9-Nitropaullone;NSC 705701; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Leost, M.,Schultz, C.,Link, A., et al. Paullones are potent inhibitors of glycogen synthase kinase-3β and cyclin-dependent kinase 5/p25. European Journal of Biochemistry 267, 5983-5994 (2000). 2.Bain, J.,McLauchlan, H.,Elliot, M., et al. The specificities of protein kinase inhibitors: An update. Biochemistry Journal 371, 199-204 (2003). 3.Trevino, M.,Stefanik, D.J.,Rodriguez, R., et al. Induction of canonical Wnt signaling by alsterpaullone is sufficient for oral tissue fate during regeneration and embryogenesis in Nematostella vectensis. Developmental Dynamics 240, 2673-2679 (2011). 4.Selenica, M.L.,Jensen, H.S.,Larsen, A.K., et al. Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation. British Journal of Pharmacology 152(6), 959-979 (2007). 5.Makhortova, N.R.,Hayhurst, M.,Cerqueira, A., et al. A screen for regulators of survival of motor neuron protein levels. Nature Chemical Biology 7(8), 544-552 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | 4 |
| 纯度 | ≥98% |
| 计算分子量 | 293.3 |
| 分子式 | C16H11N3O3 |
| CAS号 | 237430-03-4 |
| 稳定性 | ≥ 2 years |
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