Table 2 IC50 values of D1870 for kinases inhibited by BI-D1870

The indicated kinases were assayed in the presence of concentrations of BI-D1870 ranging from 1 nM to 100 μM and IC50 values were extrapolated from this data. RSK isoforms were all assayed with 100 μM ATP, as the Km for ATP for RSK3 and RSK4 have not been determined. Other kinases were assayed at the approximate Km concentration of ATP. Protein kinases were assayed as described in the Supplementary section (at http://www.BiochemJ.org/bj/401/bj4010029add.htm) and abbreviations are defined in the legend to Table 1. The results are the means±S.E.M of two separate experiments with each assay condition performed in triplicate.

Protein kinaseKinase familyATP concentration in assay (μM)IC50 (μM)
RSK1AGC1000.031±0.005
RSK2AGC1000.024±0.005
RSK3AGC1000.018±0.003
RSK4AGC1000.015±0.007
MST2STE200.86±0.028
GSK3βCMGC51.59±0.021
MARK3CaMK52.20±0.247
CK1CK1200.45±0.042
Aurora BAurora200.34±0.141
PLK1PLK500.10±0.029