In vitro activity: CP21R7 (also known CP21) is a potent and highly selective GSK-3β inhibitor that can potently activate canonical Wnt signalling with IC(50) of 0.6nM for GSK-3β. It is a maleimide analog with the incorporation of polar groups which afforded compounds with good bioavailability. CP21R7 has an IC50 of 0.6nM for GSK-3β, and is over 100-fold more selective for GSK-3β than a panel of other kinases, and CP21R7 shows efficacy in an in vivo rat osteoporosis models. The X-ray structure of GSK-3β protein with CP21R7 bound revealed the binding mode of the template and provided insights for future optimization opportunities.

Kinase Assay: CP21R7 has an IC50 of 0.6nM for GSK-3β, and is over 100-fold more selective for GSK-3β than a panel of other kinases

Cell Assay: