| Assay Method Information | |
| | The CDK8/CDK19 Inhibitor DBA-8 Rescues Proliferation of RPS19-Deficient Erythroid Progenitor Cells |
| Description: | The results presented in Example 3 and in particular the KinomeScan indicate that the activity of DBA-7 in our proliferation assay was due to inhibition of CDK8 and/or CDK19. Since DBA-4 also inhibited CDK19 (FIG. 4), we hypothesized that CDK8 and/or CDK19 is the common target of the active compounds in the thienopyridine series.To confirm CDK8 and/or CDK19 as therapeutic targets for rescuing proliferation of RPS19-deficient cells, the activity of structurally different molecules with the same kinase target profile in the proliferation rescue assay was tested. A group of selective CDK8/CDK19 inhibitors were previously described in a paper by Porter et al. (Nat. Acad. Sci. Proc. 2012, 109, 13799-13804). Compound DBA-9 (described as Senexin B in WO 2013/116786) has a very similar kinase inhibition profile as DBA-7. We therefore tested the structurally similar and commercially available CDK8/CDK19 inhibitor DBA-8 (described as Senexin A by Porter et al. 2012) in our proliferation rescue assay. |
| Affinity data for this assay | |
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