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
1Sutherland, C., Leighton, I.A., and Cohen, P.Inactivation of glycogen synthase kinase 3β by phosphorylation: New kinase connections in insulin and growth-factor signaling. Biochem J296(Pt. 1)15-19(1993).
2Papkoff, J., and Aikawa, M.WNT-1 and HGF regulate GSK3β activity and β-catenin signaling in mammary epithelial cells. Biochem Biophys Res Commun247(3)851-858(1998).
3Ring, 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. Diabetes52(3)588-95(2003).
4Li, W., Zhou, H., Abujarour, R., et al. Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells27(12)2992-3000(2009).
5Ying, Q., Wray, J., Nichols, J., et al. The ground state of embryonic stem cell self-renewal. Nature453519-524(2008).
Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.
Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.
Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
Manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research
Analytical testing services and custom synthesis also available