Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and.

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Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and.

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Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. (A) General synthetic scheme for synthesis of the pyrazolo-tetrahydroquinolinone scaffold. TFA, trifluoroacetic acid; TFE, 2,2,2-trifluoroethanol. (B) IC50 values for the inhibition of GSK3α and GSK3β were determined at Km of ATP in a motility shift microfluidic assay (Caliper) measuring phosphorylation of a synthetic substrate. Values are average of three or more experiments. Data are shown as IC50 values in μM ± SD. Compounds were tested in duplicate in a 12-point dose curve with threefold dilution starting at 33.3 μM. (C) Kinome-wide selectivity for BRD0705 and BRD3731 represented on a kinome phylogenetic tree. Each inhibitor was screened against 311 kinases at a 10 μM concentration. Kinases with >50% inhibition are depicted (percentage inhibition proportional to size of red dot). Florence F. Wagner et al., Sci Transl Med 2018;10:eaam8460 Copyright © 2018 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works