Uses
CP21R7 is a potent and selective inhibitor of GSK3β.
Biological Activity
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.
