Table 3.
Specificity of compound 2 and T-00127-HEV1 for PI4KIIIβ compared to a panel of lipid and protein kinases
| Specificitya | Compound 2 | T00127HEV1 |
|---|---|---|
| PI4KIIIB IC50 (nM) | 48 ± 5 | 140 ± 10 |
| PI4KIIIA IC50 (nM) | >10,000 | >10,000 |
| Lipid kinase panel | 2/8b | 0/8 |
| PIK3C2A IC50 (nM) | 12,000 | >10,000 |
| PIK3C2B IC50 (nM) | 5,600 | >10,000 |
| Protein kinase panel | 2/277 | 0/277 |
| STK17A IC50 (nM) | 2,100 | >10,000 |
| MSK2 IC50 (nM) | 4,600 | >10,000 |
a
The PI4KIIIβ and PI4KIIIα EC50 and CC50 data are averages of two experiments (± standard deviations). Invitrogen kinase screening was performed in duplicate at a single point of 10 μM and in dose response when active at 10 μM.
b
x/number of kinases tested indicates that compound showed activity greater than 50% against x kinases.