| 货号 | 13122-1mg |
| 描述 | Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that plays a key inhibitory role in both the insulin and Wnt signaling pathways.1,2 CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.3 When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3.3 CHIR99021 activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle.3 A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes.3 CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.4,5 |
| 别名 | CT 99021; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sutherland, C.,Leighton, I.A., and Cohen, P. Inactivation of glycogen synthase kinase 3β by phosphorylation: New kinase connections in insulin and growth-factor signaling. Biochemistry Journal 296(Pt. 1), 15-19 (1993). 2.Papkoff, J., and Aikawa, M. WNT-1 and HGF regulate GSK3β activity and β-catenin signaling in mammary epithelial cells. Biochemical and Biophysical Research Communications 247(3), 851-858 (1998). 3.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). 4.Li, W.,Zhou, H.,Abujarour, R., et al. Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells 27(12), 2992-3000 (2009). 5.Ying, Q.L.,Wray, J.,Nichols, J., et al. The ground state of embryonic stem cell self-renewal. Nature 453, 519-524 (2008). | |
| 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 | 465.3 |
| 分子式 | C22H18Cl2N8 |
| CAS号 | 252917-06-9 |
| 稳定性 | ≥ 2 years |
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