Published TCIMAIL newest issue No.197
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Glycogen Synthase Kinase (GSK) Inhibitor
No.164(January 2015)
(2'Z,3'E)-6-Bromoindirubin-3'-oxime (BIO, 1) is a cell-permeable indirubin compound and acts as an inhibitor of glycogen synthase kinase-3 (GSK-3).1,2) As shown below, the inhibitory activity of 1 is highly selective to GSK-3 in comparison with other kinases.1)
Inhibition of GSK by 1 mediates the activation of the Wnt signaling pathway and sustains pluripotency in human and mouse embryonic stem (ES) cells.3) 1 is also reported to induce the differentiation of neonatal cardiomyocytes and to maintain self-renewal in human and mouse ES cells.4)
References
- 1)GSK-3-selective inhibitors derived from Tyrian purple indirubins
- 2)Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases
- 3)Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor
- 4)The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes
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