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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Structures of CK1 inhibitors and their effects on CK1 activity in vitro. Structures of CK1 inhibitors and their effects on CK1 activity in vitro. (A) Structures.

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Fig. 7 Gel scaffold for inhibition of postsurgical recurrence of B16F10 tumors. Gel scaffold for inhibition of postsurgical recurrence of B16F10 tumors.

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Fig. 6 ROC curves of mCCNA1 and mVIM assayed on esophageal balloon samplings of the distal esophagus. ROC curves of mCCNA1 and mVIM assayed on esophageal.

Fig. 2. Best model fits. Best model fits. Illustration of the best model fits for the (A) basic, (B) continuous, and (C) cluster models. See Table 1 and.

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Fig. 3 CSF1 is expressed in human melanoma.

Fig. 8 Analysis of bone structure within the soft and stiff scaffold.

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Fig. 1 LB100 and LB102 specifically inhibit PP2A phosphatase activity and the growth of BCR-ABL+ cells. LB100 and LB102 specifically inhibit PP2A phosphatase.

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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.

Suppression of melanoma cell proliferation in response to kinase inhibitors. Suppression of melanoma cell proliferation in response to kinase inhibitors.

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by Dana S. Levy, Jason A. Kahana, and Rakesh Kumar

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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 Published by AAAS