Table 2.
In-vitro IC50 data for the isoform selective small molecule inhibitors determined in the presence of 10μM ATP. Most of this data was previously published in [17].
| Compound | PIK-23 | TGX-286 | PIK-75 | PIK-85 | PIK-90 | PIK-108 | PI-103 | PIK124 |
|---|---|---|---|---|---|---|---|---|
| PI3Ks | ||||||||
| p110α/p85α | >200 | 4.5 | 0.0058 | 0.044 | 0.011 | 2.6 | 0.0082 | 0.023 |
| p110β/p85α | 42 | 0.12 | 1.3 | 0.8 | 0.35 | 0.057 | 0.088 | 1.1 |
| p110δ/p85α | 0.097 | 1 | 0.51 | 0.08 | 0.058 | 0.26 | 0.048 | 0.34 |
| p110γ | 50 | 10 | 0.076 | 0.05 | 0.018 | 4.1 | 0.15 | 0.054 |
| PI3KC2α | >100 | >100 | ~10 | ND | 0.047 | ~100 | ~1 | 0.14 |
| PI3KC2β | 100 | ~100 | ~1 | ND | 0.064 | ~20 | 0.026 | 0.37 |
| PI3KC2y | >100 | ND | ND | ND | ND | ND | ND | ND |
| hsVPS34 | ~50 | 3.1 | 2.6 | ND | 0.83 | ~5 | 2.3 | 10 |
| PI4Ks | ||||||||
| PI4Kllα | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| PWKIIIα | >100 | >100 | >100 | 2.5 | 0.83 | ~.50 | >100 | >100 |
| PI4KIIIβ | >100 | >100 | >100 | 3.6 | 3.1 | >100 | >100 | >100 |
| PIKKs | ||||||||
| ATR | >100 | >100 | 21 | ND | 15 | >100 | 0.85 | 2 |
| ATM | >100 | >100 | 2.3 | ~50 | 0.61 | 35 | 0.92 | ND |
| DNA-PK | >100 | ~50 | 0.0017 | 0.061 | 0.013 | 0.12 | 0.0019 | 1.5 |
| mTORC1 | >100 | >100 | 1 | >100 | 1.05 | ND | 0.02 | ND |
| mTORC2 | >101 | ND | 0.16 | ND | ND | ND | 0.125 | ND |
| hSMG-1 | ND | ND | ND | ND | ND | ND | ND | ND |
| PIPKs | ||||||||
| PI4P5Klα | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| PI4P5KIβ | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| PI5P4KIIβ | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |