| 货号 | 16676-25mg |
| 描述 | The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.1 They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.2,3,4 AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).5,6 It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.5 AZD 1080 inhibits tau phosphorylation in cells.5 It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).5 In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ring, D.B.,Johnson, K.W.,Henriksen, E.J., et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes 52(3), 588-595 (2003). 2.Asuni, A.A.,Hooper, C.,Reynolds, C.H., et al. GSK3α exhibits β-catenin and tau directed kinase activities that are modulated by Wnt. European Journal of Neuroscience 24(12), 3387-3392 (2006). 3.Phiel, C.J.,Wilson, C.A.,Lee, V.M., et al. GSK-3α regulates production of Alzheimer’s disease amyloid-β peptides. Nature 423(6938), 435-439 (2003). 4.Guerrero, F.,Herencia, C.,Almadén, Y., et al. TGF-β prevents phosphate-induced osteogenesis through inhibition of BMP and Wnt/β-catenin pathways. PLoS One 9(2), e89179 (2014). 5.Georgievska, B.,Sandin, J.,Doherty, J., et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. Journal of Neurochemistry 125(3), 446-456 (2013). 6.Eldar-Finkelman, H. and Martinez, A. GSK-3 inhibitors: Preclinical and clinical focus on CNS. Front.Mol.Neurosci. 4, 1-18 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 334.4 |
| 分子式 | C19H18N4O2 |
| CAS号 | 612487-72-6 |
| 稳定性 | ≥ 2 years |
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