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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].

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