货号 | 15578-25mg |
描述 | The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylates and inactivates glycogen synthase, preventing glycogen synthesis.1 They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.2,3,4 CHIR98014 is a reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC50 = 0.65 and 0.58 nM, respectively).1 It is inactive against a series of other serine/threonine or tyrosine kinases.1 Through its effects on GSK3, CHIR98014 stimulates glycogen synthase in cells (EC50 = 106 nM), potentiates insulin-dependent glucose transport in isolated muscle strips, and improves glucose disposal in diabetic animals.1 CHIR98014 also reduces tau phosphorylation in rat brains and supports Wnt signaling during osteogenesis.5,4 |
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.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). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 486.3 |
分子式 | C20H17Cl2N9O2 |
CAS号 | 556813-39-9 |
稳定性 | ≥ 2 years |
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