CP21R7 is a potent and selective inhibitor of GSK3β.
The glycogen synthase kinase-3β (GSK-3β), a serine/threonine, is a ubiquitous kinase that participates in a multitude of cellular processes, such as cell membrane-to-nucleus signaling, gene transcription, translation, cytoskeletal structuring and cell cycle progression and survival [1].
In vitro: CP21R7 was an inhibitor of GSK3β and PKCα with the IC50 values of 1.8 and 1900 nM, respectively [1]. In the human reporter cell line, CP21R7 potently activated canonical Wnt signallingeven at the dose of 1 μM, with highest activity seen at 3 μM [2]. In human iPSCs exposed to N2B27 medium, supplemented with 1 μM GSK3β inhibitor CP21R7 strongly upregulated the expression of T (also known as Brachyury, T/BRY), a meso-endoderm marker expressed in the primitive streak [2].
References:
[1] Gong L, Hirschfeld D, Tan Y C, et al. Discovery of potent and bioavailable GSK-3β inhibitors[J]. Bioorganic & medicinal chemistry letters, 2010, 20(5): 1693-1696.
[2] Ciampi O, Iacone R, Longaretti L, et al. Generation of functional podocytes from human induced pluripotent stem cells[J]. Stem cell research, 2016, 17(1): 130-139.